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List of works by Alan P Kozikowski

1-amino-APDC, a partial agonist of group II metabotropic glutamate receptors with neuroprotective properties

scientific article published on 01 June 1999

11C-MCG: synthesis, uptake selectivity, and primate PET of a probe for glutamate carboxypeptidase II (NAALADase).

scientific article published in April 2002

18F-ZW-104: a new radioligand for imaging neuronal nicotinic acetylcholine receptors--in vitro binding properties and PET studies in baboons

scientific article published in August 2009

2,3-Disubstituted quinuclidines as a novel class of dopamine transporter inhibitors

scientific article

2,3-disubstituted 6-azabicyclo[3.2.1]octanes as novel dopamine transporter inhibitors

scientific article published in March 2004

2-Aminoadipic Acid-C(O)-Glutamate Based Prostate-Specific Membrane Antigen Ligands for Potential Use as Theranostics

scientific article published on 24 October 2018

3-(Hydroxymethyl)-bearing phosphatidylinositol ether lipid analogues and carbonate surrogates block PI3-K, Akt, and cancer cell growth

scientific article published on 01 August 2000

5-HT2C Agonists Modulate Schizophrenia-Like Behaviors in Mice.

scientific article published on 15 March 2017

A Novel Role for Histone Deacetylase 6 (HDAC6) in the Regulation of IL-10 and Immune Tolerance Mediated by Antigen-Presenting Cells (APCs). ⬇️

scholarly article

A Short and Efficient Synthesis of the Pharmacological Research Tool GW501516 for the Peroxisome Proliferator-Activated Receptor δ ⬇️

scientific article published on November 14, 2003

A convenient procedure for the synthesis of nonsymmetrical bivalent selective serotonin reuptake inhibitors using polymer-supported reagents

scientific article published on 01 December 2000

A microenvironment-mediated c-Myc/miR-548m/HDAC6 amplification loop in non-Hodgkin B cell lymphomas

scientific article

A novel role for histone deacetylase 6 in the regulation of the tolerogenic STAT3/IL-10 pathway in APCs.

scientific article

A patent review of histone deacetylase 6 inhibitors in neurodegenerative diseases (2014-2019)

scientific article published on 25 December 2019

A series of halogenated heterodimeric inhibitors of prostate specific membrane antigen (PSMA) as radiolabeled probes for targeting prostate cancer

scientific article

A series of potent and selective, triazolylphenyl-based histone deacetylases inhibitors with activity against pancreatic cancer cells and Plasmodium falciparum

scientific article

A versatile approach to PI(3,4)P2, PI(4,5)P2, and PI(3,4,5)P3 from L-(-)-quebrachitol

scientific article published on 01 January 2000

ATPS-91GSK-3 INHIBITOR 9-ING-41 ENHANCES GENOTOXIC THERAPY OF GBM LEADING TO CURE FROM INTRACRANIAL BRAIN TUMOR.

scientific article

Abstract LB-074: Priming the tumor microenvironment with epigenetic modifiers to overcome resistance to immune checkpoint inhibitors

scholarly article

Acetylenic pyridines for use in PET imaging of nicotinic receptors.

scientific article published in January 2007

Active Benzimidazole Derivatives Targeting the MmpL3 Transporter in Mycobacterium abscessus

scientific article published on 07 January 2020

Advancing the Therapeutic Potential of Indoleamides for Tuberculosis

scientific article published on 24 June 2019

An enantioselective synthesis and biobehavioral evaluation of 7-fluoro-3-(p-fluorophenyl)-2-propyltropanes

scientific article published in July 2000

An optimized RAD51 inhibitor that disrupts homologous recombination without requiring Michael acceptor reactivity.

scientific article

Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors

scientific article published on 21 July 2008

Antinociceptive effects of N-acetylaspartylglutamate (NAAG) peptidase inhibitors ZJ-11, ZJ-17 and ZJ-43 in the rat formalin test and in the rat neuropathic pain model

scientific article published on July 2004

Antinociceptive pharmacology of N-(4-chlorobenzyl)-N'-(4-hydroxy-3-iodo-5-methoxybenzyl) thiourea, a high-affinity competitive antagonist of the transient receptor potential vanilloid 1 receptor

scientific article published on 20 February 2007

Author Correction: Selective HDAC6 inhibitors improve anti-PD-1 immune checkpoint blockade therapy by decreasing the anti-inflammatory phenotype of macrophages and down-regulation of immunosuppressive proteins in tumor cells

scientific article published on 10 October 2019

Biaryl Analogues of Conformationally Constrained Tricyclic Tropanes as Potent and Selective Norepinephrine Reuptake Inhibitors: Synthesis and Evaluation of Their Uptake Inhibition at Monoamine Transporter Sites ⬇️

scientific article published on May 8, 2003

Bicyclic-Capped Histone Deacetylase 6 Inhibitors with Improved Activity in a Model of Axonal Charcot-Marie-Tooth Disease

scientific article published on 24 November 2015

Biodistribution, tumor detection, and radiation dosimetry of 18F-DCFBC, a low-molecular-weight inhibitor of prostate-specific membrane antigen, in patients with metastatic prostate cancer

scientific article published on December 2012

Biological evaluation of potent triclosan-derived inhibitors of the enoyl-acyl carrier protein reductase InhA in drug-sensitive and drug-resistant strains of Mycobacterium tuberculosis

scientific article

Brain Penetrable Histone Deacetylase 6 Inhibitor SW-100 Ameliorates Memory and Learning Impairments in a Mouse Model of Fragile X Syndrome

scientific article published on 14 December 2018

Cellular pharmacology of D-3-azido-3-deoxy-myo-inositol, an inhibitor of phosphatidylinositol signaling having antiproliferative activity

scientific article published on January 1994

Characterization of Maleimide-Based Glycogen Synthase Kinase-3 (GSK-3) Inhibitors as Stimulators of Steroidogenesis ⬇️

scientific article published on June 17, 2013

Chemical medicine: novel 10-substituted cytisine derivatives with increased selectivity for alpha4beta2 nicotinic acetylcholine receptors

scientific article published on 01 August 2007

Chemical synthesis and pharmacology of 6- and 7-hydroxylated 2-carbomethoxy-3-(p-tolyl)tropanes: antagonism of cocaine's locomotor stimulant effects

scientific article published in August 2000

Chemistry and Behavioral Studies Identify Chiral Cyclopropanes as Selective α4β2-Nicotinic Acetylcholine Receptor Partial Agonists Exhibiting an Antidepressant Profile ⬇️

scientific article published on January 10, 2012

Chemistry and Biology of the 2.beta.-Alkyl-3.beta.-phenyl Analogs of Cocaine: Subnanomolar Affinity Ligands That Suggest a New Pharmacophore Model at the C-2 Position ⬇️

scientific article published on August 4, 1995

Chemistry and Pharmacology of the Piperidine-Based Analogues of Cocaine. Identification of Potent DAT Inhibitors Lacking the Tropane Skeleton ⬇️

scientific article published on May 21, 1998

Chemistry and biology of mercaptoacetamides as novel histone deacetylase inhibitors

scientific article published on 01 March 2005

Chemistry and pharmacological characterization of novel nitrogen analogues of AMOP-H-OH (Sazetidine-A, 6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol) as α4β2-nicotinic acetylcholine receptor-selective partial agonists.

scientific article

Chemistry and pharmacology of nicotinic ligands based on 6-[5-(azetidin-2-ylmethoxy)pyridin-3-yl]hex-5-yn-1-ol (AMOP-H-OH) for possible use in depression

scientific article

Chemistry, Pharmacology, and Behavioral Studies Identify Chiral Cyclopropanes as Selective α4β2-Nicotinic Acetylcholine Receptor Partial Agonists Exhibiting an Antidepressant Profile. Part II ⬇️

scientific article published on June 26, 2013

Chemistry, biology, and QSAR studies of substituted biaryl hydroxamates and mercaptoacetamides as HDAC inhibitors-nanomolar-potency inhibitors of pancreatic cancer cell growth

scientific article published on March 2008

Chiral Mercaptoacetamides Display Enantioselective Inhibition of Histone Deacetylase 6 and Exhibit Neuroprotection in Cortical Neuron Models of Oxidative Stress

scientific article published on 10 January 2012

CoMFA study of piperidine analogues of cocaine at the dopamine transporter: exploring the binding mode of the 3 alpha-substituent of the piperidine ring using pharmacophore-based flexible alignment

scientific article

Cocaine and dopamine differentially protect [3H]mazindol binding sites from alkylation by N-ethylmaleimide

scientific article published on December 1, 1992

Combination Treatment with the GSK-3 Inhibitor 9-ING-41 and CCNU Cures Orthotopic Chemoresistant Glioblastoma in Patient-Derived Xenograft Models

scientific article

Complete (1)H NMR spectral fingerprint of huperzine A.

scientific article published in October 2007

Continuous Activity Assay for HDAC11 Enabling Reevaluation of HDAC Inhibitors

scientific article published on 15 November 2019

Controlling Extra- and Intramacrophagic Mycobacterium abscessus by Targeting Mycolic Acid Transport

scientific article

Defining the minimal structural requirements for partial agonism at the type I myo-inositol 1,4,5-trisphosphate receptor

scientific article published on 01 February 1997

Derivatives of 3-isoxazolecarboxylic acid esters: a potent and selective compound class against replicating and nonreplicating Mycobacterium tuberculosis

scientific article published on January 2012

Design and Discovery of Functionally Selective Serotonin 2C (5-HT2C) Receptor Agonists

scientific article

Design and Synthesis of (2-(5-Chloro-2,2-dimethyl-2,3-dihydrobenzofuran-7-yl)cyclopropyl)methanamine as a Selective Serotonin 2C Agonist

scientific article published on June 2015

Design and Synthesis of Aryl Ether Inhibitors of theBacillus AnthracisEnoyl-ACP Reductase

scientific article

Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands

scientific article published on 13 April 2020

Design and Synthesis of Mercaptoacetamides as Potent, Selective, and Brain Permeable Histone Deacetylase 6 Inhibitors

scientific article published on 7 April 2017

Design and synthesis of 2-pyridones as novel inhibitors of the Bacillus anthracis enoyl-ACP reductase.

scientific article published on 4 May 2008

Design and synthesis of a PSMA inhibitor-doxorubicin conjugate for targeted prostate cancer therapy

scientific article published on March 2006

Design and synthesis of a potent and selective peptidomimetic inhibitor of caspase-3.

scientific article

Design of a high-affinity competitive antagonist of the vanilloid receptor selective for the calcium entry-linked receptor population

scientific article published in February 2004

Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT2C) receptor agonist without 5-HT2B agonism

scientific article published on 14 August 2019

Design of remarkably simple, yet potent urea-based inhibitors of glutamate carboxypeptidase II (NAALADase)

scientific article (publication date: February 2001)

Design, Synthesis, and Pharmacological Evaluation of Mefloquine-Based Ligands as Novel Antituberculosis Agents

scientific article published on 01 November 2007

Design, Synthesis, and SAR Studies of Mefloquine-Based Ligands as Potential Antituberculosis Agents

scientific article published on 01 June 2006

Development of Small Molecules that Specifically Inhibit the D-loop Activity of RAD51.

scientific article

Development of new brain imaging agents based upon nocaine-modafinil hybrid monoamine transporter inhibitors

scientific article (publication date: 15 June 2006)

Differential binding and dopamine uptake activity of cocaine analogues modified at nitrogen

scholarly article

Dipolar Cycloaddition Route to Diverse Analogues of Cocaine: The 6- and 7-Substituted 3-Phenyltropanes ⬇️

scientific article published on 01 February 1997

Discovery of Highly Potent and Selective α4β2-Nicotinic Acetylcholine Receptor (nAChR) Partial Agonists Containing an Isoxazolylpyridine Ether Scaffold that Demonstrate Antidepressant-like Activity. Part II ⬇️

scientific article published on November 2, 2012

Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications.

scientific article

Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models

scientific article published on 04 September 2019

Discovery of isoxazole analogues of sazetidine-A as selective α4β2-nicotinic acetylcholine receptor partial agonists for the treatment of depression

scientific article

Discovery of novel conformationally constrained tropane-based biaryl and arylacetylene ligands as potent and selective norepinephrine transporter inhibitors and potential antidepressants

scientific article published in May 2005

Discrimination of potent inhibitors of Toxoplasma gondii enoyl-acyl carrier protein reductase by a thermal shift assay

scientific article published on 13 December 2013

Dissociation between duration of action in the forced swim test in mice and nicotinic acetylcholine receptor occupancy with sazetidine, varenicline, and 5-I-A85380.

scientific article published on 13 April 2011

Divergent roles of histone deacetylase 6 (HDAC6) and histone deacetylase 11 (HDAC11) on the transcriptional regulation of IL10 in antigen presenting cells

scientific article

Dopaminergic agents for the treatment of cocaine abuse

scientific article

Dual function glutamate-related ligands: discovery of a novel, potent inhibitor of glutamate carboxypeptidase II possessing mGluR3 agonist activity

scientific article

Dysregulation of glutamate carboxypeptidase II in psychiatric disease.

scientific article published on 10 January 2008

Enantiopure Cyclopropane-Bearing Pyridyldiazabicyclo[3.3.0]octanes as Selective α4β2-nAChR Ligands

scientific article

Epigenetic regulation of autophagy by the methyltransferase G9a

scientific journal article

Evaluation of Protein Kinase Inhibitors with PLK4 Cross-Over Potential in a Pre-Clinical Model of Cancer ⬇️

scientific article published on 29 April 2019

Exploration of the labeling of [11C]tubastatin A at the hydroxamic acid site with [11C]carbon monoxide.

scientific article

From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells

scientific article published on April 2009

From serendipity to rational antituberculosis drug discovery of mefloquine-isoxazole carboxylic acid esters

scientific article published in November 2009

From α4β2 Nicotinic Ligands to the Discovery of σ1 Receptor Ligands: Pharmacophore Analysis and Rational Design.

scientific article published on December 2012

Functional differences in epigenetic modulators-superiority of mercaptoacetamide-based histone deacetylase inhibitors relative to hydroxamates in cortical neuron neuroprotection studies

scientific article

Functionalization of the alicyclic skeleton of epibatidine: synthesis and nicotinic acetylcholine receptor binding affinities of epibatidine analogues

scientific article

Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.

scientific article published on 24 December 2015

Further SAR studies of piperidine-based analogues of cocaine. 2. Potent dopamine and serotonin reuptake inhibitors

scientific article (publication date: 23 March 2000)

Further studies on conformationally constrained tricyclic tropane analogues and their uptake inhibition at monoamine transporter sites: synthesis of (Z)-9-(substituted arylmethylene)-7-azatricyclo[4.3.1.0(3,7)]decanes as a novel class of serotonin t

scientific article

GSK-3 inhibition overcomes chemoresistance in human breast cancer

scientific article published on 14 July 2016

GSK-3β Governs Inflammation-Induced NFATc2 Signaling Hubs to Promote Pancreatic Cancer Progression

scientific article published on 28 January 2016

Glutamate carboxypeptidase II levels in rodent brain using [125I]DCIT quantitative autoradiography

scientific article published in October 2005

Glycogen Synthase Kinase-3 Inhibition Sensitizes Pancreatic Cancer Cells to Chemotherapy by Abrogating the TopBP1/ATR-Mediated DNA Damage Response

scientific article published on 18 September 2019

HDAC6 inhibition promotes α-tubulin acetylation and ameliorates CMT2A peripheral neuropathy in mice

scientific article published on 05 March 2020

HDAC6 inhibitors reverse axonal loss in a mouse model of mutant HSPB1–induced Charcot-Marie-Tooth disease

article

HDAC6 is a target for protection and regeneration following injury in the nervous system

scientific article

HDAC6 is a therapeutic target in mutant GARS-induced Charcot-Marie-Tooth disease.

scientific article published on 5 February 2018

HTS and rational drug design to generate a class of 5-HT(2C)-selective ligands for possible use in schizophrenia

scientific article

HTS, chemical hybridization, and drug design identify a chemically unique antituberculosis agent-coupling serendipity and rational approaches to drug discovery

scientific article published in June 2007

Highly potent and specific GSK-3beta inhibitors that block tau phosphorylation and decrease alpha-synuclein protein expression in a cellular model of Parkinson's disease.

scientific article published on February 2006

Histone deacetylase 6 and heat shock protein 90 control the functions of Foxp3(+) T-regulatory cells

scientific article

Histone deacetylase 6 inhibition improves memory and reduces total tau levels in a mouse model of tau deposition.

scientific article

Histone/protein deacetylase 11 targeting promotes Foxp3+ Treg function.

scientific article

Identification and Development of Novel Inhibitors of Toxoplasma gondii Enoyl Reductase

scientific article

Identification of HDAC6-Selective Inhibitors of Low Cancer Cell Cytotoxicity

scientific article

Identification of Novel α4β2-Nicotinic Acetylcholine Receptor (nAChR) Agonists Based on an Isoxazole Ether Scaffold that Demonstrate Antidepressant-like Activity ⬇️

scientific article published on January 4, 2012

Identification of a Glycogen Synthase Kinase‐3β Inhibitor that Attenuates Hyperactivity in CLOCK Mutant Mice ⬇️

scientific article published on July 5, 2011

Identification of a Maleimide-Based Glycogen Synthase Kinase-3 (GSK-3) Inhibitor, BIP-135, that Prolongs the Median Survival Time of Δ7 SMA KO Mouse Model of Spinal Muscular Atrophy.

scientific article published on January 2012

Identification, synthesis, and pharmacological evaluation of tetrahydroindazole based ligands as novel antituberculosis agents

scientific article published in January 2010

In pursuit of natural product leads: synthesis and biological evaluation of 2-[3-hydroxy-2-[(3-hydroxypyridine-2-carbonyl)amino]phenyl]benzoxazole-4-carboxylic acid (A-33853) and its analogues: discovery of N-(2-benzoxazol-2-ylphenyl)benzamides as n

scientific article

Indole-2-carboxamide-based MmpL3 Inhibitors Show Exceptional Antitubercular Activity in an Animal Model of Tuberculosis Infection

scientific article published on 8 June 2016

Indoleamides are active against drug-resistant Mycobacterium tuberculosis

scientific article published on January 2013

Inhibition of GSK-3 induces differentiation and impaired glucose metabolism in renal cancer.

scientific article published on 10 December 2013

Insights into the structural determinants required for high-affinity binding of chiral cyclopropane-containing ligands to α4β2-nicotinic acetylcholine receptors: an integrated approach to behaviorally active nicotinic ligands

scientific article

Interactions between human glutamate carboxypeptidase II and urea-based inhibitors: structural characterization

scientific article

Intracerebroventricular administration of N-acetylaspartylglutamate (NAAG) peptidase inhibitors is analgesic in inflammatory pain

scientific article published on August 2008

Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity

scientific article published on 20 April 2009

Isoxazolyl-serine-based agonists of peroxisome proliferator-activated receptor: design, synthesis, and effects on cardiomyocyte differentiation

scientific article published in December 2004

Ketamine and N-acetylaspartylglutamate peptidase inhibitor exert analgesia in bone cancer pain

scientific article published in September 2006

Local administration of N-acetylaspartylglutamate (NAAG) peptidase inhibitors is analgesic in peripheral pain in rats

scientific article

Mercaptoacetamide: A promising zinc-binding group for the discovery of selective histone deacetylase 6 inhibitors

scientific article published on 29 September 2020

Methoxylation of cocaine reduces binding affinity and produces compounds of differential binding and dopamine uptake inhibitory activity: discovery of a weak cocaine "antagonist".

scientific article published in November 1993

Mixed cocaine agonist/antagonist properties of (+)-methyl 4beta-(4-chlorophenyl)-1-methylpiperidine-3alpha-carboxylate, a piperidine-based analog of cocaine

scientific article

Modeling, chemistry, and biology of the benzolactam analogues of indolactam V (ILV). 2. Identification of the binding site of the benzolactams in the CRD2 activator-binding domain of PKCdelta and discovery of an ILV analogue of improved isozyme sele

scientific article published on 01 April 1997

Modification of the side chain of micromolide, an anti-tuberculosis natural product

scientific article published in October 2008

Modification of triclosan scaffold in search of improved inhibitors for enoyl-acyl carrier protein (ACP) reductase in Toxoplasma gondii

scientific article published on 14 June 2013

Molecular Basis for the Selective Inhibition of Histone Deacetylase 6 by a Mercaptoacetamide Inhibitor

scientific article published on 21 November 2018

Molecular Pathways: Revisiting Glycogen Synthase Kinase-3β as a Target for the Treatment of Cancer

scientific article published on 4 January 2017

Molecular modeling of the interactions of glutamate carboxypeptidase II with its potent NAAG-based inhibitors

scientific article

Molecular modeling, structure--activity relationships and functional antagonism studies of 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketones as a novel class of dopamine transporter inhibitors.

scientific article

Molecular modeling, synthesis, and activity studies of novel biaryl and fused-ring BACE1 inhibitors

scientific article

Mutation of Rv2887, a marR-like gene, confers Mycobacterium tuberculosis resistance to an imidazopyridine-based agent.

scientific article

N-[N-[(S)-1,3-Dicarboxypropyl]carbamoyl]-4-[18F]fluorobenzyl-L-cysteine, [18F]DCFBC: a new imaging probe for prostate cancer

scientific article published on May 2008

N-phenylalkyl-substituted tropane analogs of boat conformation with high selectivity for the dopamine versus serotonin transporter

scientific article published on 01 December 1999

NAAG peptidase inhibition reduces locomotor activity and some stereotypes in the PCP model of schizophrenia via group II mGluR.

scientific article

NAAG peptidase inhibitor increases dialysate NAAG and reduces glutamate, aspartate and GABA levels in the dorsal hippocampus following fluid percussion injury in the rat.

scientific article published on 5 April 2006

NAAG peptidase inhibitor reduces acute neuronal degeneration and astrocyte damage following lateral fluid percussion TBI in rats

scientific article

NAAG peptidase inhibitors and their potential for diagnosis and therapy

scientific article

NOC chemistry for tuberculosis-further investigations on the structure-activity relationships of antitubercular isoxazole-3-carboxylic acid ester derivatives

scientific article published on October 2010

Natural product leads for drug discovery: isolation, synthesis and biological evaluation of 6-cyano-5-methoxyindolo[2,3-a]carbazole based ligands as antibacterial agents ⬇️

scientific article published on 4 September 2009

Neuroprotective and nootropic actions of a novel cyclized dipeptide after controlled cortical impact injury in mice

scientific article published in March 2003

New amide-bearing benzolactam-based protein kinase C modulators induce enhanced secretion of the amyloid precursor protein metabolite sAPPalpha

scientific article published on January 2003

New bivalent PKC ligands linked by a carbon spacer: enhancement in binding affinity

scientific article published in September 2003

Novel HDAC inhibitors with radiosensitizing properties

scientific article

Novel N-benzoyl-2-hydroxybenzamide disrupts unique parasite secretory pathway

scientific article

Novel PI analogues selectively block activation of the pro-survival serine/threonine kinase Akt.

scientific article

Novel Peptidomimetic Cysteine Protease Inhibitors as Potential Antimalarial Agents

scientific article published on 01 June 2006

Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter

scientific article

Novel diketopiperazine enhances motor and cognitive recovery after traumatic brain injury in rats and shows neuroprotection in vitro and in vivo

scientific article published in March 2003

Novel inhibitors of human histone deacetylase (HDAC) identified by QSAR modeling of known inhibitors, virtual screening, and experimental validation

scientific article

Novel monoamine transporter ligands reduce cocaine-induced enhancement of brain stimulation reward

scientific article

Novel pyridyl ring C5 substituted analogues of epibatidine and 3-(1-methyl-2(S)-pyrrolidinylmethoxy)pyridine (A-84543) as highly selective agents for neuronal nicotinic acetylcholine receptors containing beta2 subunits

scientific article

Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents

scientific article published on 10 February 2015

Optimization of Drug Candidates That Inhibit the D-Loop Activity of RAD51

scientific article published on 17 April 2019

Palladium catalyzed synthesis of annelated indoles ⬇️

scholarly article

Peroxisome proliferator-activated receptor delta and gamma agonists differentially alter tumor differentiation and progression during mammary carcinogenesis

scientific article

Pharmacokinetics and brain penetration of LF-3-88, (2-[5-[5-(2(S)-azetidinylmethoxyl)-3-pyridyl]-3-isoxazolyl]ethanol), a selective α4β2-nAChR partial agonist and promising antidepressant

scientific article published on 23 November 2012

Pharmacological and behavioral analysis of the effects of some bivalent ligand-based monoamine reuptake inhibitors

scientific article (publication date: 10 May 2001)

Pharmacophore-based discovery of 3,4-disubstituted pyrrolidines as a novel class of monoamine transporter inhibitors.

scientific article

Phencyclidine and dizocilpine induced behaviors reduced by N-acetylaspartylglutamate peptidase inhibition via metabotropic glutamate receptors

scientific article

Phosphatidylinositol ether lipid analogues induce AMP-activated protein kinase-dependent death in LKB1-mutant non small cell lung cancer cells

scientific article published on January 2008

Phosphatidylinositol ether lipid analogues that inhibit AKT also independently activate the stress kinase, p38alpha, through MKK3/6-independent and -dependent mechanisms.

scientific article

Physical Interaction of Histone Deacetylase 6 (HDAC6) with STAT3 Regulates IL-10 Gene Expression and Immune Tolerance Mediated by Antigen-Presenting Cells (APCs) ⬇️

scholarly article

Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization.

scientific article

Preferential inhibition of Akt and killing of Akt-dependent cancer cells by rationally designed phosphatidylinositol ether lipid analogues

scientific article published on April 2004

Preliminary structure-activity relationships and biological evaluation of novel antitubercular indolecarboxamide derivatives against drug-susceptible and drug-resistant Mycobacterium tuberculosis strains

scientific article published on 3 May 2013

Probing the binding of indolactam-V to protein kinase C through site-directed mutagenesis and computational docking simulations

scientific article published on 01 September 1999

Putting the 'HAT' back on survival signalling: the promises and challenges of HDAC inhibition in the treatment of neurological conditions

scientific article published on 01 May 2009

Pyrido[1,2-a]benzimidazole-based agents active against tuberculosis (TB), multidrug-resistant (MDR) TB and extensively drug-resistant (XDR) TB

scientific article

RI-1: a chemical inhibitor of RAD51 that disrupts homologous recombination in human cells

scientific article

Radiolabeled small-molecule ligands for prostate-specific membrane antigen: in vivo imaging in experimental models of prostate cancer

scientific article

Rational Design of Suprastat, a Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models

scientific article published on 20 August 2020

Rational Drug Design Leading to the Identification of a Potent 5-HT(2C) Agonist Lacking 5-HT(2B) Activity

scientific article

Rational design and development of radiation-sensitizing histone deacetylase inhibitors

scientific article published on November 2005

Rational design and simple chemistry yield a superior, neuroprotective HDAC6 inhibitor, tubastatin A

scientific article

Rational design of 5-phenyl-3-isoxazolecarboxylic acid ethyl esters as growth inhibitors of Mycobacterium tuberculosis. a potent and selective series for further drug development

scientific article published in January 2010

Recent Developments Using Small Molecules to Target RAD51: How to Best Modulate RAD51 for Anticancer Therapy?

scientific article

Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors

scientific article

Role of the increased noradrenergic neurotransmission in drug self-administration

scientific article

SAR studies of piperidine-based analogues of cocaine. 4. Effect of N-modification and ester replacement

scientific article (publication date: 18 July 2002)

Sar studies of piperidine-based analogues of cocaine. Part 3: oxadiazoles

scientific article (publication date: 20 August 2001)

Sazetidine-A, a novel ligand that desensitizes alpha4beta2 nicotinic acetylcholine receptors without activating them

scientific article

Searching for disease modifiers-PKC activation and HDAC inhibition - a dual drug approach to Alzheimer's disease that decreases Abeta production while blocking oxidative stress

scientific article

Searching for new cures for tuberculosis: design, synthesis, and biological evaluation of 2-methylbenzothiazoles

scientific article published in November 2009

Second-generation histone deacetylase 6 inhibitors enhance the immunosuppressive effects of Foxp3+ T-regulatory cells

scientific article published on 5 January 2012

Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action

scientific article

Selective HDAC6 inhibitors improve anti-PD-1 immune checkpoint blockade therapy by decreasing the anti-inflammatory phenotype of macrophages and down-regulation of immunosuppressive proteins in tumor cells

scientific article published on 16 April 2019

Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth.

scientific article

Spectrum of activity and molecular correlates of response to phosphatidylinositol ether lipid analogues, novel lipid-based inhibitors of Akt.

scientific article published on March 2006

Stereochemistry at the forefront in the design and discovery of novel anti-tuberculosis agents

scientific article published on January 2011

Stereoselective HDAC inhibition from cysteine-derived zinc-binding groups.

scientific article published in August 2009

Structural analogs of huperzine A improve survival in guinea pigs exposed to soman

scientific article published in December 2012

Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor

scientific article published on 15 January 2020

Structural basis of RasGRP binding to high-affinity PKC ligands.

scientific article published in February 2002

Structural remodeling of cocaine: design and synthesis of trisubstituted cyclopropanes as selective serotonin reuptake inhibitors

scientific article published in January 2006

Structure-activity relationship studies of N-sulfonyl analogs of cocaine: role of ionic interaction in cocaine binding

scientific article published in September 1994

Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue

scientific article published on December 11, 1992

Structure-activity relationships for a series of quinoline-based compounds active against replicating and nonreplicating Mycobacterium tuberculosis.

scientific article

Structure-activity relationships of compounds targeting mycobacterium tuberculosis 1-deoxy-D-xylulose 5-phosphate synthase

scientific article

Structure-based design leads to the identification of lithium mimetics that block mania-like effects in rodents. possible new GSK-3beta therapies for bipolar disorders

scientific article

Structure-guided design of a highly selective glycogen synthase kinase-3β inhibitor: a superior neuroprotective pyrazolone showing antimania effects

scientific article

Studies in polyphenol chemistry and bioactivity. 4.(1) Synthesis of trimeric, tetrameric, pentameric, and higher oligomeric epicatechin-derived procyanidins having all-4beta,8-interflavan connectivity and their inhibition of cancer cell growth throu

scientific article published in March 2003

Studies of benzamide- and thiol-based histone deacetylase inhibitors in models of oxidative-stress-induced neuronal death: identification of some HDAC3-selective inhibitors

scientific article published in May 2009

Synergistic interactions of indole-2-carboxamides and β-lactam antibiotics against Mycobacterium abscessus

scientific article published on 10 February 2020

Synthesis and Akt inhibitory properties of a 1d-3,4-dideoxyphosphatidylinositol ether lipid ⬇️

scholarly article

Synthesis and Behavioral Studies of Chiral Cyclopropanes as Selective α4β2-Nicotinic Acetylcholine Receptor Partial Agonists Exhibiting an Antidepressant Profile. Part III.

scientific article published in April 2016

Synthesis and Biology of the Conformationally Restricted ACPD Analogue, 2-Aminobicyclo[2.1.1]hexane-2,5-dicarboxylic Acid-I, a Potent mGluR Agonist ⬇️

scientific article published on May 7, 1998

Synthesis and Pharmacological Evaluation of Selective Histone Deacetylase 6 Inhibitors in Melanoma Models

scientific article published on 5 September 2017

Synthesis and anticholinesterase activity of huperzine A analogues containing phenol and catechol replacements for the pyridone ring

scientific article published on 01 June 1998

Synthesis and biological activity of novel neuroprotective diketopiperazines

scientific article

Synthesis and biological evaluation of 1-azabicyclo-[3.2.1]octanes: new dopamine transporter inhibitors

scientific article published on 01 August 2000

Synthesis and biological evaluation of novel hybrids of highly potent and selective α4β2-Nicotinic acetylcholine receptor (nAChR) partial agonists.

scientific article

Synthesis and biological evaluation of triazol-4-ylphenyl-bearing histone deacetylase inhibitors as anticancer agents

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Synthesis and biological evaluation of two analogues of (S)-alpha-methyl-3-carboxyphenylalanine

scientific article published on 01 September 1998

Synthesis and biological evaluation of two novel DAT-binding technetium complexes containing a piperidine based analogue of cocaine

scientific article published in November 1999

Synthesis and biological properties of new 2beta-alkyl- and 2beta-aryl-3-(substituted phenyl)tropane derivatives: stereochemical effect of C-3 on affinity and selectivity for neuronal dopamine and serotonin transporters

scientific article published in December 1998

Synthesis and biology of 1D-3-deoxyphosphatidylinositol: a putative antimetabolite of phosphatidylinositol-3-phosphate and an inhibitor of cancer cell colony formation

scientific article published on 01 March 1995

Synthesis and biology of a 7-nitro-2,1,3-benzoxadiazol-4-yl derivative of 2-phenylindole-3-acetamide: a fluorescent probe for the peripheral-type benzodiazepine receptor

scientific article published on 01 August 1997

Synthesis and evaluation of iodine-123 labelled tricyclic tropanes as radioligands for the serotonin transporter

scientific article published in October 2003

Synthesis and evaluation of technetium-99m- and rhenium-labeled inhibitors of the prostate-specific membrane antigen (PSMA).

scientific article

Synthesis and metabotropic glutamate receptor activity of a 2-aminobicyclo[3.2.0]heptane-2,5-dicarboxylic acid, a molecule possessing an extended glutamate conformation

scientific article published on 01 April 1998

Synthesis and metabotropic receptor activity of the novel rigidified glutamate analogues (+)- and (-)-trans-azetidine-2,4-dicarboxylic acid and their N-methyl derivatives

scientific article published on 01 September 1993

Synthesis and modeling study of (2S,5R,6R)- and (2S,5R,6S)-6-hydroxy- 8-(1-decynyl)-benzolactam-V8 as protein kinase C modulators

scientific article published on 01 June 2002

Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors

scientific article published in April 2004

Synthesis and pharmacological evaluation of ( Z )-9-(Heteroarylmethylene)-7-azatricyclo[4.3.1.0 3,7 ]decanes: thiophene analogues as potent norepinephrine transporter inhibitors ⬇️

scientific article published on October 20, 2003

Synthesis and pharmacological evaluation of 8- and 9-substituted benzolactam-v8 derivatives as potent ligands for protein kinase C, a therapeutic target for Alzheimer's disease

scientific article published on 01 March 2006

Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity

scientific article published on May 2006

Synthesis and protein kinase C binding activity of benzolactam-V7

scientific article published on 01 May 1999

Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications

scientific article

Synthesis of 7-substituted benzolactam-V8s and their selectivity for protein kinase C isozymes

scientific article published on 01 July 2002

Synthesis of 8-Oxa analogues of norcocaine endowed with interesting cocaine-like activity.

scientific article published in July 1999

Synthesis of more potent analogues of the acetylcholinesterase inhibitor, huperzine B

scientific article published on 01 June 2002

Synthesis of novel spirocyclic cocaine analogs using the Suzuki coupling

Synthesis of the benzofuran analogue of ILV, a new protein kinase C (PKC) activator

scholarly article

Synthesis of urea-based inhibitors as active site probes of glutamate carboxypeptidase II: efficacy as analgesic agents

scientific article published in March 2004

Synthesis, biological evaluation, and structure-activity relationships for 5-[(E)-2-arylethenyl]-3-isoxazolecarboxylic acid alkyl ester derivatives as valuable antitubercular chemotypes.

scientific article

Synthesis, biological evaluation, and structure-activity relationships of N-benzoyl-2-hydroxybenzamides as agents active against P. falciparum (K1 strain), Trypanosomes, and Leishmania

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Synthesis, chiral chromatographic separation, and biological activities of the enantiomers of 10,10-dimethylhuperzine A

scientific article published on 01 November 2000

Synthesis, molecular modeling, and biological studies of novel piperidine-based analogues of cocaine: evidence of unfavorable interactions proximal to the 3alpha-position of the piperidine ring

scientific article

Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues

scientific article published on March 2003

Targeting Mycolic Acid Transport by Indole-2-carboxamides for the Treatment of Mycobacterium abscessus Infections.

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The RAD51-stimulatory compound RS-1 can exploit the RAD51 overexpression that exists in cancer cells and tumors

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The amino terminus of tau inhibits kinesin-dependent axonal transport: implications for filament toxicity.

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The novel triple reuptake inhibitor JZAD-IV-22 exhibits an antidepressant pharmacological profile without locomotor stimulant or sensitization properties

scientific article

The potent and selective α4β2*/α6*-nicotinic acetylcholine receptor partial agonist 2-[5-[5-((S)Azetidin-2-ylmethoxy)-3-pyridinyl]-3-isoxazolyl]ethanol demonstrates antidepressive-like behavior in animal models and a favorable ADME-tox profile.

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The preclinical candidate indole-2-carboxamide improves immune responses to Mycobacterium tuberculosis infection in healthy subjects and individuals with type 2 diabetes

scholarly article by Ruoqiong Cao et al published 19 June 2019 in International Microbiology

Thiol-Based Potent and Selective HDAC6 Inhibitors Promote Tubulin Acetylation and T-Regulatory Cell Suppressive Function

scientific article published on 5 October 2015

Thiophene derivatives: a new series of potent norepinephrine and serotonin reuptake inhibitors

scientific article published in April 2002

Tubastatin A, an HDAC6 inhibitor, alleviates stroke-induced brain infarction and functional deficits: potential roles of α-tubulin acetylation and FGF-21 up-regulation

scientific article published on 21 January 2016

Use of molecular modeling, docking, and 3D-QSAR studies for the determination of the binding mode of benzofuran-3-yl-(indol-3-yl)maleimides as GSK-3beta inhibitors

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Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.

scientific article

Utilization of an in vivo reporter for high throughput identification of branched small molecule regulators of hypoxic adaptation

scientific article published on April 2010

We Need 2C but Not 2B: Developing Serotonin 2C (5-HT2C) Receptor Agonists for the Treatment of CNS Disorders.

scientific article published on 28 October 2015

Why Hydroxamates May Not Be the Best Histone Deacetylase Inhibitors--What Some May Have Forgotten or Would Rather Forget?

scientific article published on 25 November 2015

Why academic drug discovery makes sense

scientific article

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