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List of works by Gunda I. Georg

(3R,5S,7as)-(3,5-Bis(4-fluorophenyl)tetrahydro-1H-oxazolo[3,4-c]oxazol-7a-yl)methanol, a novel neuroprotective agent

scientific article published on December 2009

4-Deacetyltaxol and 10-acetyl-4-deacetyltaxotere: synthesis and biological evaluation

scientific article published on 01 November 1994

A Message from the Editors-in-Chief

scientific article published on 22 February 2019

A One-Flask Synthesis of Weinreb Amides from Chiral and Achiral Carboxylic Acids Using the Deoxo-Fluor Fluorinating Reagent

article

A Special Issue on Contraceptive Development: Past, Present, and Future

scientific article published on 24 July 2020

A concise formal total synthesis of lactimidomycin

scientific article published on 01 May 2015

A convenient method for the efficient removal of ruthenium byproducts generated during olefin metathesis reactions

scientific article published on 01 May 2001

A convenient method to remove ruthenium byproducts from olefin metathesis reactions using polymer-bound triphenylphosphine oxide (TPPO).

scientific article published in January 2005

A high-throughput screen utilizing the fluorescence of riboflavin for identification of lumazine synthase inhibitors

scientific article published in March 2005

A novel lumazine synthase inhibitor derived from oxidation of 1,3,6,8-tetrahydroxy-2,7-naphthyridine to a tetraazaperylenehexaone derivative

scientific article published on 10 March 2007

A novel potent indazole carboxylic acid derivative blocks spermatogenesis and is contraceptive in rats after a single oral dose

scientific article

A one-step synthesis of a deuterated paclitaxel analogue: 10-deacetoxy-(10alpha-2H)paclitaxel

scientific article published on 01 December 1999

A preclinical evaluation of Minnelide as a therapeutic agent against pancreatic cancer

scientific article published on October 2012

A systematic SAR study of C10 modified paclitaxel analogues using a combinatorial approach

scientific article

Absolute quantitative (1)h NMR spectroscopy for compound purity determination.

scientific article published on 7 November 2014

Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors

scientific article

Advances toward COVID-19 Therapies Special Issue Call for Papers

scientific article published on 02 December 2020

Allosteric Modulators of Drug Targets Special Issue.

scientific article published on 7 February 2018

Alzheimer's disease special thematic issue: call for papers.

scientific article published on 29 March 2012

Amino acid-derived enaminones: a study in ring formation providing valuable asymmetric synthons

scientific article

Amyloid peptide toxicity and microtubule-stabilizing drugs.

scientific article

Artificial Intelligence in Drug Discovery: Into the Great Wide Open

scientific article published on 08 July 2020

Artificial neural network--based analysis of high-throughput screening data for improved prediction of active compounds

scientific article

BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen.

scientific article

BET proteins: Investigating BRDT as a potential target for male contraception

scientific article published on 21 January 2020

Biomimetic Aerobic C-H Olefination of Cyclic Enaminones at Room Temperature: Development toward the Synthesis of 1,3,5-Trisubstituted Benzenes

scientific article

Boron-Heck reaction of cyclic enaminones: regioselective direct arylation via oxidative palladium(II) catalysis

scientific article published on 03 March 2014

Butitaxel analogues: synthesis and structure-activity relationships

scientific article published on 01 January 1997

Characterizing the Epothilone Binding Site on β-Tubulin by Photoaffinity Labeling: Identification of β-Tubulin Peptides TARGSQQY and TSRGSQQY as Targets of an Epothilone Photoprobe for Polymerized Tubulin

scientific article published on 17 March 2016

Chemical modification of paclitaxel (Taxol) reduces P-glycoprotein interactions and increases permeation across the blood-brain barrier in vitro and in situ

scientific article published in February 2005

Chemoenzymatic synthesis of cryptophycin/arenastatin natural products

scientific article

Chirally Pure Prodrugs and Their Converting Enzymes Lead to High Supersaturation and Rapid Transcellular Permeation of Benzodiazepines

scientific article published on 22 June 2016

Conformationally restricted paclitaxel analogues: macrocyclic mimics of the "hydrophobic collapse" conformation

scientific article published on 01 October 1999

Confronting Racism in Chemistry Journals

scientific article published on 19 June 2020

Confronting Racism in Chemistry Journals

Cooperativity Between Orthosteric Inhibitors and Allosteric Inhibitor 8-Anilino-1-Naphthalene Sulfonic Acid (ANS) in Cyclin-Dependent Kinase 2

scientific article published on 20 May 2020

Copper-assisted palladium(II)-catalyzed direct arylation of cyclic enaminones with arylboronic acids

scientific article published on 22 October 2012

Correction to BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen

scientific article

Cryptophycin affinity labels: synthesis and biological activity of a benzophenone analogue of cryptophycin-24.

scientific article published on February 2003

Current Medicinal Chemistry Research in India: Progress and Opportunities

scientific article

Cyclin-Dependent Kinase Inhibitor Dinaciclib Interacts with the Acetyl-Lysine Recognition Site of Bromodomains

scientific article

DFG-1 Binding: A New Residue for Developing Selective Kinase Inhibitors

scientific article published on 11 September 2020

Dehydrogenative alkenylation of uracils via palladium-catalyzed regioselective C-H activation.

scientific article published on 25 March 2013

Design, Synthesis, and Characterization of a Fluorescence Polarization Pan-BET Bromodomain Probe

scientific article published on 31 October 2018

Design, Synthesis, and in Vitro and in Vivo Evaluation of Ouabain Analogues as Potent and Selective Na,K-ATPase α4 Isoform Inhibitors for Male Contraception

scientific article published in January 2018

Design, synthesis, and antiproliferative and CDK2-cyclin a inhibitory activity of novel flavopiridol analogues.

scientific article

Development of Highly Potent and Selective Diaminothiazole Inhibitors of Cyclin-Dependent Kinases

scientific article

Development of WEE2 kinase inhibitors as novel non-hormonal female contraceptives that target meiosis†

scientific article published on 12 June 2020

Digital chemistry in the Journal of Medicinal Chemistry.

scientific article

Direct Hiyama cross-coupling of enaminones with triethoxy(aryl)silanes and dimethylphenylsilanol

scientific article published on 22 September 2011

Discovery and development of a small molecule library with lumazine synthase inhibitory activity

scientific article published in August 2009

Discovery and development of the covalent hydrates of trifluoromethylated pyrazoles as riboflavin synthase inhibitors with antibiotic activity against Mycobacterium tuberculosis

scientific journal article

Discovery of a Potential Allosteric Ligand Binding Site in CDK2

scientific article

Diversity-Oriented Library Synthesis from Steviol and Isosteviol-Derived Scaffolds

scientific article published on 17 February 2020

Drug Annotations for a New Decade

scientific article published on 22 January 2020

Drug Metabolism and Toxicology Special Issue Call for Papers

scientific article published on 11 January 2019

Efficient and practical asymmetric synthesis of the taxol C-13 side chain, N-benzoyl-(2R,3S)-3-phenylisoserine, and its analogs via chiral 3-hydroxy-4-aryl-.beta.-lactams through chiral ester enolate-imine cyclocondensation

Enantioselective synthesis of 3,4-dihydro-1,2-oxazepin-5(2H)-ones and 2,3-dihydropyridin-4(1H)-ones from β-substituted β-hydroxyaminoaldehydes

scientific article published on 13 January 2014

Enantioselective synthesis of a 3'-dephenylcryptophycin synthon

scientific article published on 01 November 1998

Enantiospecific Synthesis and Biological Investigations of a Nuphar Alkaloid: Proposed Structure of a Castoreum Component.

scientific article

Enantiospecific Synthesis and Cytotoxicity Evaluation of Oximidine II Analogues.

scientific article published on 31 May 2016

Enantiospecific formal total syntheses of (-)-salicylihalamides A and B from D-glucose and L-rhamnose

scientific article published on 01 October 2003

Enantiospecific synthesis and cytotoxicity of 7-(4-methoxyphenyl)-6-phenyl-2,3,8,8a-tetrahydroindolizin-5(1H)-one enantiomers

scientific article published on 4 March 2008

Endocrine disruption by indole-3-carbinol and tamoxifen: blockage of ovulation.

scientific article published in September 2002

Epigenetics 2.0: Special Issue on Epigenetics-Call for Papers

scientific article published on 22 October 2020

Epigenetics: Novel Therapeutics Targeting Epigenetics

scientific article published on 29 January 2016

Epigenetics: novel therapeutics targeting epigenetics

scientific article published on 22 December 2014

Epothilone and paclitaxel: unexpected differences in promoting the assembly and stabilization of yeast microtubules

scientific article published in March 2002

Formal total syntheses of the (-)-salicylihalamides A and B from D-glucose and L-rhamnose

scientific article

Formal total synthesis of (+)-salicylihalamides A and B: a combined chiral pool and RCM strategy

scientific article published in December 2003

From HTS to Phase I: the Institute for Therapeutics Discovery and Development at the University of Minnesota

scientific article published in March 2014

From dioxin to drug lead--the development of 2,3,7,8-tetrachlorophenothiazine

scientific article published on June 2007

Gamendazole, an orally active indazole carboxylic acid male contraceptive agent, targets HSP90AB1 (HSP90BETA) and EEF1A1 (eEF1A), and stimulates Il1a transcription in rat Sertoli cells

scientific journal article

Halohydrin analogues of cryptophycin 1: synthesis and biological activity.

scientific article

Heme Binding Biguanides Target Cytochrome P450-Dependent Cancer Cell Mitochondria

scientific article published on 01 October 2017

Heme Binding Biguanides Target Cytochrome P450-Dependent Cancer Cell Mitochondria.

scientific article

Hepatitis C virus (HCV) therapies special thematic issue: call for papers.

scientific article published on 7 January 2013

High-throughput screening for growth inhibitors using a yeast model of familial paraganglioma

scientific article

Human Adenine Nucleotide Translocase (ANT) Modulators Identified by High-Throughput Screening of Transgenic Yeast

scientific article published on 8 January 2016

Identification and Screening of Selective WEE2 Inhibitors to Develop Non-Hormonal Contraceptives that Specifically Target Meiosis

scientific article published on 05 December 2019

Identification of the Metabolic Profile of the α-Tubulin-Binding Natural Product (-)-Pironetin

scientific article published on 29 January 2019

Inducing Protein Degradation as a Therapeutic Strategy.

scientific article published on 20 May 2016

Intranasal Coadministration of a Diazepam Prodrug with a Converting Enzyme Results in Rapid Absorption of Diazepam in Rats

scientific article published on 05 March 2019

Introduction: Drug Metabolism and Toxicology Special Issue

scientific article published on 02 June 2020

Investigation of 3'-debenzoyl-3'-(3-([¹²⁴I]-iodobenzoyl))paclitaxel analog as a radio-tracer to study multidrug resistance in vivo.

scientific article

Ionic immobilization, diversification, and release: application to the generation of a library of methionine aminopeptidase inhibitors

scientific article

Lithium Perchlorate-, Acetic Anhydride-, and Triphenylphosphine-assisted Multicomponent Syntheses of 4-Unsubstituted 2,5-Dioxooctahydroquinoline-3-carboxylates and 3-carbonitriles

scientific article published on 05 September 2013

Microwave-assisted Suzuki-Miyaura couplings on α-iodoenaminones

scientific article

Mild and selective hydrozirconation of amides to aldehydes using Cp2Zr(H)Cl: scope and mechanistic insight

scientific article

N-Butyldeoxygalactonojirimycin Induces Reversible Infertility in Male CD Rats

scientific article published on 31 December 2019

N-methylation of the c3' amide of taxanes: synthesis of N-methyltaxol C and N-methylpaclitaxel

scientific article published on 23 May 2008

New Horizons in Drug Discovery - Understanding and Advancing Kinase Inhibitors

scientific article published on 15 July 2020

Novel d-seco paclitaxel analogues: synthesis, biological evaluation, and model testing.

scientific article

Novel endotoxin-sequestering compounds with terephthalaldehyde-bis-guanylhydrazone scaffolds

scientific article published on 11 January 2006

Novel prodrug approach for tertiary amines: synthesis and preliminary evaluation of N-phosphonooxymethyl prodrugs

scientific article published on 01 August 1999

Ongoing in vivo studies with cytoskeletal drugs in tau transgenic mice.

scientific article published on July 2006

Overcoming the blood-brain barrier to taxane delivery for neurodegenerative diseases and brain tumors.

scientific article published in January 2003

Paclitaxel succinate analogs: Anionic and amide introduction as a strategy to impart blood-brain barrier permeability

scientific article

Palladium(II)-catalyzed dehydrogenative alkenylation of cyclic enaminones via the Fujiwara-Moritani reaction

scientific article published on 13 October 2011

Palladium(II)-catalyzed direct arylation of enaminones using organotrifluoroborates

scientific article published on 6 March 2008

Palladium-catalyzed direct C-H arylation of cyclic enaminones with aryl iodides

scientific article published on 10 June 2013

Pharmacological activity of retinoic acid receptor alpha-selective antagonists in vitro and in vivo

scientific article published on May 2013

Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts

scientific article

Potent Pyrimidine and Pyrrolopyrimidine Inhibitors of Testis-Specific Serine/Threonine Kinase 2 (TSSK2).

scientific article published on 26 September 2017

Preparation and physicochemical characterization of a novel water-soluble prodrug of carbamazepine.

scientific article

Protection against beta-amyloid toxicity in primary neurons by paclitaxel (Taxol)

scientific article published on 01 April 1998

Rapid delivery of diazepam from supersaturated solutions prepared using prodrug/enzyme mixtures: toward intranasal treatment of seizure emergencies

scientific article

Rapid entry into the cryptophycin core via an acyl-beta-lactam macrolactonization: total synthesis of cryptophycin-24

scientific article published on 01 June 2001

Recombinant production of enzymatically active male contraceptive drug target hTSSK2 - Localization of the TSKS domain phosphorylated by TSSK2

scientific article

Reformulating Tylocrebrine in Epidermal Growth Factor Receptor Targeted Polymeric Nanoparticles Improves Its Therapeutic Index

scientific article published on 3 July 2015

Regioselective C5-alkylation and C5-methylcarbamate formation of 2,3-dihydro-4-pyridones and C3-alkylation and C3-methylcarbamate formation of 4-(pyrrolidin-1-yl)furan-2(5H)-one

scientific article

Retinoic acid receptor antagonists for male contraception: Current status

scientific article published on 15 July 2020

Review of rationale and progress towards targeting cyclin-dependent kinase 2 (CDK2) for male contraception1

scientific article published on 16 June 2020

Revisiting microtubule targeting agents: α-Tubulin and the pironetin binding site as unexplored targets for cancer therapeutics

scientific article published on 21 May 2019

Scalable syntheses of the BET bromodomain inhibitor JQ1.

scientific article published on June 2015

Single-site chemical modification at C10 of the baccatin III core of paclitaxel and Taxol C reduces P-glycoprotein interactions in bovine brain microvessel endothelial cells

scientific article

Site-specifically traced drug release and biodistribution of a paclitaxel-antibody conjugate toward improvement of the linker structure.

scientific article

Stability of the human Hsp90-p50Cdc37 chaperone complex against nucleotides and Hsp90 inhibitors, and the influence of phosphorylation by casein kinase 2

scientific article published on 19 January 2015

Stabilization of the cyclin-dependent kinase 5 activator, p35, by paclitaxel decreases beta-amyloid toxicity in cortical neurons.

scientific article published on January 2003

Structural Basis of ALDH1A2 Inhibition by Irreversible and Reversible Small Molecule Inhibitors

scientific article published on 14 December 2017

Structural basis of Wee kinases functionality and inactivation by diverse small molecule inhibitors

scientific article published on 09 August 2017

Structure-Activity Studies of N-Butyl-1-deoxynojirimycin (NB-DNJ) Analogues: Discovery of Potent and Selective Aminocyclopentitol Inhibitors of GBA1 and GBA2.

scientific article published on 3 October 2017

Studies toward the synthesis of oximidines I and II

scientific article published on 01 December 2003

Studies towards the synthesis of methionine aminopeptidase inhibitors: diversification utilizing a ROMP-derived coupling reagent.

scientific article

Support vector machines in HTS data mining: Type I MetAPs inhibition study

scientific article

Syntheses of PDE3A inhibitor ORG9935 and determination of the absolute stereochemistries of its enantiomers by X-ray crystallography.

scientific article published on 18 April 2018

Synthesis and Cytotoxicity Evaluation of C4- and C5-Modified Analogues of the α,β-Unsaturated Lactone of Pironetin

scientific article

Synthesis and Spectral Properties of 8-Anilinonaphthalene-1-sulfonic Acid (ANS) Derivatives Prepared by Microwave-Assisted Copper(0)-Catalyzed Ullmann Reaction

scientific article published on 28 October 2019

Synthesis and anti-tubulin activity of a 3'-(4-azidophenyl)-3'-dephenylpaclitaxel photoaffinity probe

scientific article published in December 2004

Synthesis and evaluation of C2 functionalized analogs of the α-tubulin-binding natural product pironetin

scientific article published on 11 November 2017

Synthesis and evaluation of eight- and four-membered iminosugar analogues as inhibitors of testicular ceramide-specific glucosyltransferase, testicular β-glucosidase 2, and other glycosidases

scientific article published on 20 March 2012

Synthesis and evaluation of heteroaromatic 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1H)-ones for cytotoxicity against the HCT-116 colon cancer cell line

scientific article

Synthesis and evaluation of the anti-proliferative and NF-κB activities of a library of simplified tylophorine analogs

scientific article

Synthesis and interactions of 7-deoxy-, 10-deacetoxy, and 10-deacetoxy-7-deoxypaclitaxel with NCI/ADR-RES cancer cells and bovine brain microvessel endothelial cells

scientific article published on 3 November 2005

Synthesis of 6- and 7-membered cyclic enaminones: scope and mechanism

scientific article

Synthesis of Arylazide- and Diazirine-Containing CrAsH-EDT2 Photoaffinity Probes

scientific article published on 7 March 2016

Synthesis of Arylazide- and Diazirine-Containing CrAsH-EDT2 Photoaffinity Probes: Unfortunately, in the article

scientific article published on 01 July 2016

Synthesis of Strained 1,3-Diene Macrocycles via Copper-Mediated Castro-Stephens Coupling/Alkyne Reduction Tandem Reactions

scientific article published on 15 July 2015

Synthesis of a quinolone library from ynones

scientific article

Synthesis of amino acid derived enaminones via Wolff rearrangement using vinylogous amides as carbon nucleophiles

scientific article

Synthesis of biologically active taxol analogues with modified phenylisoserine side chains

scientific article published on October 30, 1992

Synthesis of cryptophycins via an N-acyl-beta-lactam macrolactonization

scientific article

Synthesis of docetaxel and butitaxel analogues through kinetic resolution of racemic beta-lactams with 7-O-triethylsilylbaccatin III.

scientific article published on February 2007

Synthesis of fused bicyclic systems with nitrogen atom at the bridgehead, including indolizidines and quinolizidines

scientific article published on 31 March 2011

Synthesis of oximidine II by a copper-mediated reductive ene-yne macrocyclization

scientific article published on 29 June 2011

Synthesis of skeletally diverse and stereochemically complex library templates derived from isosteviol and steviol

scientific article

Synthesis of tylocrebrine and related phenanthroindolizidines by VOF3-mediated oxidative aryl-alkene coupling

scientific article published on 14 December 2010

Synthesis, Conformational Analysis, and Biological Evaluation of Heteroaromatic Taxanes

scientific article published on April 1996

Synthesis, in vitro and in vivo cytotoxicity of 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1H)-ones

scientific article

Synthesis, modeling, and anti-tubulin activity of a D-seco paclitaxel analogue

scientific article published in February 2004

Synthesis, tubulin assembly, and antiproliferative activity against MCF7 and NCI/ADR-RES cancer cells of 10-O-acetyl-5'-hydroxybutitaxel

scientific article published on 07 October 2008

Synthetic studies with 13-deoxybaccatin III.

scientific article published in October 2002

The 2020 Nobel Prize in Physiology or Medicine

scientific article published on 05 November 2020

The Ecstasy and Agony of Assay Interference Compounds

scientific article

The Ecstasy and Agony of Assay Interference Compounds

The Ecstasy and Agony of Assay Interference Compounds

The Ecstasy and Agony of Assay Interference Compounds

scientific article published on 28 February 2017

The Ecstasy and Agony of Assay Interference Compounds

The Ecstasy and Agony of Assay Interference Compounds

scientific article published in 2017

The Ecstasy and Agony of Assay Interference Compounds

The Ecstasy and Agony of Assay Interference Compounds.

scientific article published on 28 February 2017

The Fungal Sexual Pheromone Sirenin Activates the Human CatSper Channel Complex

scientific article published on 16 December 2015

The Future Is Now: Artificial Intelligence in Drug Discovery

scientific article published on 23 May 2019

The Future of Drug Repositioning

The Na+ and K+ transport system of sperm (ATP1A4) is essential for male fertility and an attractive target for male contraception†

scientific article published on 16 June 2020

The anti-parasitic agent suramin and several of its analogues are inhibitors of the DNA binding protein Mcm10

scientific article published on 14 August 2019

The cryptophycins: their synthesis and anticancer activity

scientific article

The effect of the aromatic rings of taxol on biological activity and solution conformation: synthesis and evaluation of saturated taxol and taxotere analogues

scientific article published on 01 September 1994

The oxetane conformational lock of paclitaxel: structural analysis of D-secopaclitaxel.

scientific article

The use of polymer-bound triphenylphosphine in the stereochemical inversion of secondary alcohols

scientific article published on 01 April 2000

Three-component synthesis of cyclic enaminones via ketene cyclization

scientific article

Total Syntheses and Cytotoxicity of (R)- and (S)-Boehmeriasin A.

scientific article

Total syntheses of arylindolizidine alkaloids (+)-ipalbidine and (+)-antofine

scientific article

Total synthesis and anti-tubulin activity of epi-c3 analogues of cryptophycin-24.

scientific article published on July 2004

Total synthesis and antitubulin activity of c10 analogues of cryptophycin-24.

scientific article published on January 2004

Total synthesis and evaluation of 22-(3-azidobenzoyloxy)methyl epothilone C for photoaffinity labeling of beta-tubulin

scientific article

Total synthesis and evaluation of C25-benzyloxyepothilone C for tubulin assembly and cytotoxicity against MCF-7 breast cancer cells.

scientific article

Total synthesis and evaluation of C26-hydroxyepothilone D derivatives for photoaffinity labeling of beta-tubulin.

scientific article

Transition in Leadership: Opportunities and Challenges

scientific article published on December 22, 2011

Ultra-High-Throughput Screening of Natural Product Extracts to Identify Proapoptotic Inhibitors of Bcl-2 Family Proteins.

scientific article

Understanding tubulin-Taxol interactions: mutations that impart Taxol binding to yeast tubulin

scientific article

Update to Our Reader, Reviewer, and Author Communities-April 2020

scientific article published on 22 April 2020

Update to Our Reader, Reviewer, and Author Communities-April 2020

scientific article published on 23 April 2020

Wallifoliol, a taxol congener with a novel carbon skeleton, from Himalayan Taxus wallichiana

scientific article published on 01 June 1994

Water-soluble benzodiazepine prodrug/enzyme combinations for intranasal rescue therapies

scientific article

Women in Medicinal Chemistry Special Issue Call for Papers

scientific article published on 05 April 2019

Women in Medicinal Chemistry: Ad Maiora!

scientific article published on 20 February 2020

[Bis(2-methoxyethyl)amino]sulfur trifluoride, the Deoxo-Fluor reagent: application toward one-flask transformations of carboxylic acids to amides

scientific article published in April 2004

{beta}-Amyloid-induced neurodegeneration and protection by structurally diverse microtubule-stabilizing agents.

scientific article published on 16 September 2004