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List of works by Bill Denny

3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel

scientific article published on 15 February 2019

3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3

scientific article

4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione Inhibitors of the Checkpoint Kinase Wee1. Structure−Activity Relationships for Chromophore Modification and Phenyl Ring Substitution

article

4-Pyridylanilinothiazoles that selectively target von Hippel-Lindau deficient renal cell carcinoma cells by inducing autophagic cell death.

scientific article

4-anilino-5-carboxamido-2-pyridone derivatives as noncompetitive inhibitors of mitogen-activated protein kinase kinase

scientific article

6-Cyano Analogues of Bedaquiline as Less Lipophilic and Potentially Safer Diarylquinolines for Tuberculosis

scientific article

6-Nitro-2,3-dihydroimidazo[2,1-b][1,3]thiazoles: Facile synthesis and comparative appraisal against tuberculosis and neglected tropical diseases.

scientific article published on 27 March 2017

7-Substituted 2-Nitro-5,6-dihydroimidazo[2,1-b][1,3]oxazines: Novel Antitubercular Agents Lead to a New Preclinical Candidate for Visceral Leishmaniasis.

scientific article published on May 2017

A Selective and Slowly Reversible Inhibitor of l-Type Amino Acid Transporter 1 (LAT1) Potentiates Antiproliferative Drug Efficacy in Cancer Cells

scientific article published on 2 June 2016

A diacridine derivative that binds by bisintercalation at two contiguous sites on DNA

scientific article published in July 1985

A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types ⬇️

scientific article published on August 15, 2011

A mitochondria-selective near-infrared-emitting fluorescent dye for cellular imaging studies

scientific article published on 03 May 2018

A molecule targeting VHL-deficient renal cell carcinoma that induces autophagy

scientific article

A new class of quinoline-based DNA hypomethylating agents reactivates tumor suppressor genes by blocking DNA methyltransferase 1 activity and inducing its degradation

scientific article

A new selective pharmacological enhancer of the Orai1 Ca2+ channel reveals roles for Orai1 in smooth and skeletal muscle functions

scientific article published on 13 January 2020

A phase I trial of PR-104, a nitrogen mustard prodrug activated by both hypoxia and aldo-keto reductase 1C3, in patients with solid tumors.

scientific article

A roadmap for drug discovery and its translation to small molecule agents in clinical development for tuberculosis treatment

scientific article published on August 2008

Activation of 3-amino-1,2,4-benzotriazine 1,4-dioxide antitumor agents to oxidizing species following their one-electron reduction

scientific article published in January 2003

Amsacrine as a Topoisomerase II Poison: Importance of Drug–DNA Interactions ⬇️

scientific article published on February 10, 2012

An SAR study of hydroxy-trifluoromethylpyrazolines as inhibitors of Orai1-mediated store operated Ca 2+ entry in MDA-MB-231 breast cancer cells using a convenient Fluorescence Imaging Plate Reader assay

scientific article published on 09 May 2018

An improved synthesis of 5,6-dimethylxanthenone-4-acetic acid (DMXAA).

scientific article

Anionic carbonato and oxalato cobalt(III) nitrogen mustard complexes.

scientific article published on 20 January 2004

Antimalarial 9-anilinoacridine compounds directed at hematin

scientific article published on December 2003

Antitubercular Nitroimidazoles Revisited: Synthesis and Activity of the Authentic 3-Nitro Isomer of Pretomanid

scientific article

Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides

scientific article published on 27 October 2017

Aziridinyldinitrobenzamides: synthesis and structure-activity relationships for activation by E. coli nitroreductase.

scientific article published on June 2004

Benzenesulphonamide inhibitors of the cytolytic protein perforin.

scientific article published on 23 December 2016

Beta-Testing of PI3-Kinase Inhibitors: Is Beta Better? ⬇️

scientific article published on May 1, 2012

Biarylmethoxy 2-nitroimidazooxazine antituberculosis agents: Effects of proximal ring substitution and linker reversal on metabolism and efficacy.

scientific article

Biological characterization of SN32976, a selective inhibitor of PI3K and mTOR with preferential activity to PI3Kα, in comparison to established pan PI3K inhibitors

scientific article published on 9 May 2017

COMMENTARY. Pre-emptive Nutrition: Refining the Targets of Drugs Targeted to Colorectal Cancer

scientific article

Cell type-specific, topoisomerase II-dependent inhibition of hypoxia-inducible factor-1alpha protein accumulation by NSC 644221.

scientific article published on February 2007

Characterisation of radicals formed by the triazine 1,4-dioxide hypoxia-activated prodrug, SN30000.

scientific article published on 16 April 2014

Characterization of radicals formed following enzymatic reduction of 3-substituted analogues of the hypoxia-selective cytotoxin 3-amino-1,2,4-benzotriazine 1,4-dioxide (tirapazamine).

scientific article published in March 2010

Combined neutron and X-ray diffraction studies of DNA in crystals and solutions

article

Combining properties of different classes of PI3Kα inhibitors to understand the molecular features that confer selectivity.

scientific article

Comparison of hematin-targeting properties of pynacrine, an acridine analog of the benzonaphthyridine antimalarial pyronaridine

scientific article published on 16 September 2014

Corrigendum: Repurposing the Chemical Scaffold of the Anti-Arthritic Drug Lobenzarit to Target Tryptophan Biosynthesis in Mycobacterium tuberculosis

scientific article published on 11 March 2015

Creation and screening of a multi-family bacterial oxidoreductase library to discover novel nitroreductases that efficiently activate the bioreductive prodrugs CB1954 and PR-104A.

scientific article

Cross-bridged cyclen or cyclam Co(III) complexes containing cytotoxic ligands as hypoxia-activated prodrugs.

scientific article published on 17 June 2013

Crystal structure of 9-amino-N-[2-(4-morpholinyl)ethyl]-4-acridinecarboxamide bound to d(CGTACG)2: implications for structure-activity relationships of acridinecarboxamide topoisomerase poisons

scientific article

Cyclic Tetrapeptides from Nature and Design: A Review of Synthetic Methodologies, Structure, and Function

scientific article published on 16 August 2019

DNA and the chromosome - varied targets for chemotherapy

scientific article

DNA-targeted 1,2,4-benzotriazine 1,4-dioxides: potent analogues of the hypoxia-selective cytotoxin tirapazamine

scientific article published on January 2004

Demonstration by real-time polymerase chain reaction that cellular DNA alkylation by novel aminoindoline compounds affects expression of the protooncogene c-myc

scientific article

Determination of the Hypnotic Potency in Rats of the Novel Ketamine Ester Analogue SN 35210.

scientific article

Development and evaluation of PIK75 nanosuspension, a phosphatidylinositol-3-kinase inhibitor

scientific article

Development of (6 R)-2-Nitro-6-[4-(trifluoromethoxy)phenoxy]-6,7-dihydro-5 H-imidazo[2,1- b][1,3]oxazine (DNDI-8219): A New Lead for Visceral Leishmaniasis.

scientific article published on 20 February 2018

Development of PIK-75 nanosuspension formulation with enhanced delivery efficiency and cytotoxicity for targeted anti-cancer therapy.

scientific article published on 28 April 2013

Development of Rapidly Metabolized and Ultra-Short-Acting Ketamine Analogs

scientific article published on 27 March 2015

Diarylthiophenes as inhibitors of the pore-forming protein perforin

scientific article published on 7 December 2015

Dihydrofuro[3,4-c]pyridinones as inhibitors of the cytolytic effects of the pore-forming glycoprotein perforin

scientific article

Discovery of pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors.

scientific article

Effect of common and experimental anti-tuberculosis treatments on Mycobacterium tuberculosis growing as biofilms

scientific article

Effect of common and experimental anti-tuberculosis treatments on Mycobacterium tuberculosis growing as biofilms

scientific article published on 20 October 2016

Effect of nitroreduction on the alkylating reactivity and cytotoxicity of the 2,4-dinitrobenzamide-5-aziridine CB 1954 and the corresponding nitrogen mustard SN 23862: distinct mechanisms of bioreductive activation.

scientific article published on April 2003

Effect of wet milling process on the solid state of indomethacin and simvastatin.

scientific article

Effects of anticancer drugs on transcription factor-DNA interactions.

scientific article

Enhanced conversion of DNA radical damage to double strand breaks by 1,2,4-benzotriazine 1,4-dioxides linked to a DNA binder compared to tirapazamine

scientific article published in November 2003

Epigenetic regulation of gene expression as an anticancer drug target

scientific article published on 01 February 2011

Evaluation of a crystalline nanosuspension: polymorphism, process induced transformation and in vivo studies

scientific article published on 25 January 2011

Evaluation of known and novel inhibitors of Orai1-mediated store operated Ca2+ entry in MDA-MB-231 breast cancer cells using a Fluorescence Imaging Plate Reader assay.

scientific article published on 7 November 2016

Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling.

scientific article published on June 2007

Evidence that phospholipase C is involved in the antitumour action of NSC768313, a new thieno[2,3-b]pyridine derivative

scientific article published on 10 March 2016

Exploration of a series of 5-arylidene-2-thioxoimidazolidin-4-ones as inhibitors of the cytolytic protein perforin

scientific article

Exploring the isoform selectivity of TGX-221 related pyrido[1,2-a]pyrimidinone-based Class IA PI 3-kinase inhibitors: synthesis, biological evaluation and molecular modelling

scientific article

Formulation and pharmacokinetics of lipid nanoparticles of a chemically sensitive nitrogen mustard derivative: Chlorambucil

scientific article

Fragmentation of the quinoxaline N-oxide bond to the ˙OH radical upon one-electron bioreduction

scientific article published on 01 November 2014

Frameshift mutations induced by four isomeric nitroacridines and their des-nitro counterpart in the lacZ reversion assay in Escherichia coli

scientific article published in March 2006

Gemcitabine sensitization by checkpoint kinase 1 inhibition correlates with inhibition of a Rad51 DNA damage response in pancreatic cancer cells

scientific article

Genotoxicity of non-covalent interactions: DNA intercalators

scientific article published on 6 April 2007

Giving Anemia a Boost with Inhibitors of Prolyl Hydroxylase ⬇️

scientific article published on March 12, 2012

Heptamethine cyanine dye mediated drug delivery: Hype or Hope

scientific article published on 12 June 2020

Heteroaryl ether analogues of an antileishmanial 7-substituted 2-nitroimidazooxazine lead afford attenuated hERG risk: In vitro and in vivo appraisal

scientific article published on 10 October 2020

Homobivalent Conjugation Increases the Allosteric Effect of 9-aminoacridine at the α1-Adrenergic Receptors

scientific article published on 30 November 2016

Human α1-adrenoceptor subtype selectivity of substituted homobivalent 4-aminoquinolines

scientific article published on 16 September 2014

Hypoxia-activated prodrugs in cancer therapy: progress to the clinic

scientific article published on March 2010

Hypoxia-activated prodrugs: substituent effects on the properties of nitro seco-1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (nitroCBI) prodrugs of DNA minor groove alkylating agents.

scientific article published on November 2009

Hypoxia-selective 3-alkyl 1,2,4-benzotriazine 1,4-dioxides: the influence of hydrogen bond donors on extravascular transport and antitumor activity

scientific article published on 6 December 2007

Hypoxic selectivity and solubility--investigating the properties of A-ring substituted nitro seco-1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-ones (nitroCBIs) as hypoxia-activated prodrugs for antitumor therapy.

scientific article published on 8 June 2010

Improved potency of the hypoxic cytotoxin tirapazamine by DNA-targeting

scientific article

In vitro and in vivo characterization of XR11576, a novel, orally active, dual inhibitor of topoisomerase I and II.

scientific article published in January 2002

In vitro susceptibility of Trichomonas vaginalis to AT-specific minor groove binding drugs

scientific article

Inhibition of strigolactone receptors by N-phenylanthranilic acid derivatives: Structural and functional insights.

scientific article published on 9 March 2018

Inhibition of the Cytolytic Protein Perforin Prevents Rejection of Transplanted Bone Marrow Stem Cells in Vivo

scientific article published on 26 September 2019

Inhibition of the cellular function of perforin by 1-amino-2,4-dicyanopyrido[1,2-a]benzimidazoles.

scientific article published on 18 May 2011

Inhibition of the pore-forming protein perforin by a series of aryl-substituted isobenzofuran-1(3H)-ones ⬇️

scientific article published on December 22, 2011

Intermediates in the reduction of the antituberculosis drug PA-824, (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine, in aqueous solution

scientific article

Investigation into Improving the Aqueous Solubility of the Thieno[2,3-b]pyridine Anti-Proliferative Agents.

scientific article

KEA-1010, a ketamine ester analogue, retains analgesic and sedative potency but is devoid of Psychomimetic effects

scientific article published on 19 December 2019

Ketamine esters and amides as short-acting anaesthetics: Structure-activity relationships for the side-chain

scientific article published on 05 February 2019

Kinetic studies of the binding of acridinecarboxamide topoisomerase poisons to DNA: implications for mode of binding of ligands with uncharged chromophores

scientific article published in February 2002

L-Type amino acid transporter 1 (lat1)-mediated targeted delivery of perforin inhibitors

scientific article published on 15 December 2015

Long-chain triazolyl acids as inhibitors of osteoclastogenesis

scientific article published on 16 May 2013

Mass spectrometry studies of the binding of the minor groove-directed alkylating agent alkamin to AT-tract oligonucleotides.

scientific article

Mechanism of action and preclinical antitumor activity of the novel hypoxia-activated DNA cross-linking agent PR-104.

scientific article

Microtubule-stabilizing properties of the avocado-derived toxins (+)-(R)-persin and (+)-(R)-tetrahydropersin in cancer cells and activity of related synthetic analogs

scientific article published on 12 March 2016

Mode of cell death induced in Chinese hamster cells by sequence-selective DNA minor groove binding nitrogen mustards: comparison with untargeted mustards and with Hoechst 33342.

scientific article published in January 2003

Morpholylureas are a new class of potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase (AKR1C3)

scientific article

N-alkylated cyclen cobalt(III) complexes of 1-(chloromethyl)-3-(5,6,7-trimethoxyindol-2-ylcarbonyl)-2,3-dihydro-1H-pyrrolo[3,2-f]quinolin-5-ol DNA alkylating agent as hypoxia-activated prodrugs.

scientific article

Nitro seco analogues of the duocarmycins containing sulfonate leaving groups as hypoxia-activated prodrugs for cancer therapy.

scientific article

Nitroacridines with selective toxicity towards hypoxic mammalian cells: Synthesis and stability of tritiated derivatives

scientific article published in October 1985

Nitroarylmethylcarbamate prodrugs of doxorubicin for use with nitroreductase gene-directed enzyme prodrug therapy

scientific article

Non-covalent ligand/DNA interactions: minor groove binding agents

scientific article published on 6 April 2007

Novel angular benzophenazines: dual topoisomerase I and topoisomerase II inhibitors as potential anticancer agents

scientific article published on January 2002

Novel pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR ⬇️

scientific article published on November 25, 2011

Novel pyrazolo[1,5-a]pyridines with improved aqueous solubility as p110α-selective PI3 kinase inhibitors

scientific article published on 25 November 2016

Optimization of the auxiliary ligand shell of Cobalt(III)(8-hydroxyquinoline) complexes as model hypoxia-selective radiation-activated prodrugs.

scientific article published on September 2004

Oxidation of 2-deoxyribose by benzotriazinyl radicals of antitumor 3-amino-1,2,4-benzotriazine 1,4-dioxides

scientific article

PARP inhibitor cyanine dye conjugate with enhanced cytotoxic and antiproliferative activity in patient derived glioblastoma cell lines

scientific article published on 08 May 2020

Pharmacokinetic/pharmacodynamic model-guided identification of hypoxia-selective 1,2,4-benzotriazine 1,4-dioxides with antitumor activity: the role of extravascular transport

scientific article published on 15 November 2007

Pharmacokinetic/pharmacodynamic modeling identifies SN30000 and SN29751 as tirapazamine analogues with improved tissue penetration and hypoxic cell killing in tumors

scientific article

Phenazine-1-carboxamides: structure-cytotoxicity relationships for 9-substituents and changes in the H-bonding pattern of the cationic side chain

scientific article published on 10 October 2005

Phosphatidylinositol 3-kinase inhibitor (PIK75) containing surface functionalized nanoemulsion for enhanced drug delivery, cytotoxicity and pro-apoptotic activity in ovarian cancer cells

scientific article

Phosphoinositide 3-kinase α inhibitors: a patent review

scientific article published on 14 March 2013

Phosphoinositide-3-kinase (PI3K) inhibitors: identification of new scaffolds using virtual screening.

scientific article

Phosphoinositide-3-kinases (PI3Ks): combined comparative modeling and 3D-QSAR to rationalize the inhibition of p110alpha

scientific article

Potentiation of the cytotoxicity of the anticancer agent tirapazamine by benzotriazine N-oxides: the role of redox equilibria

scientific article published in January 2006

Quantitation of bystander effects in nitroreductase suicide gene therapy using three-dimensional cell cultures.

scientific article published in March 2002

Quinazolines as novel anti-inflammatory histone deacetylase inhibitors.

scientific article

Radical properties governing the hypoxia-selective cytotoxicity of antitumor 3-amino-1,2,4-benzotriazine 1,4-dioxides.

scientific article

Re-evaluating pretomanid analogues for Chagas disease: Hit-to-lead studies reveal both in vitro and in vivo trypanocidal efficacy

scientific article published on 18 September 2020

Recent developments in anticancer drug delivery using cell penetrating and tumor targeting peptides.

scientific article published on 3 February 2017

Release of nitrite from the antitubercular nitroimidazole drug PA-824 and analogues upon one-electron reduction in protic, non-aqueous solvent

scientific article published on 4 November 2009

Repositioning Antitubercular 6-Nitro-2,3-dihydroimidazo[2,1-b][1,3]oxazoles for Neglected Tropical Diseases: Structure-Activity Studies on a Preclinical Candidate for Visceral Leishmaniasis.

scientific article published on 22 February 2016

Repurposing the chemical scaffold of the anti-arthritic drug Lobenzarit to target tryptophan biosynthesis in Mycobacterium tuberculosis

scientific article

Selective Treatment of Hypoxic Tumor Cells In Vivo: Phosphate Pre‐Prodrugs of Nitro Analogues of the Duocarmycins ⬇️

scientific article published on February 17, 2011

Small-molecule CSF1R kinase inhibitors; review of patents 2015-present

scientific article published on 28 October 2020

Spin trapping of radicals other than the *OH radical upon reduction of the anticancer agent tirapazamine by cytochrome P450 reductase

scientific article published in October 2009

Structural characterisation of bisintercalation in higher-order DNA at a junction-like quadruplex

scientific article

Structure of 9-amino-[N-(2-dimethylamino)propyl]acridine-4-carboxamide bound to d(CGTACG)(2): a comparison of structures of d(CGTACG)(2) complexed with intercalatorsin the presence of cobalt

scientific article published on 21 April 2004

Structure of the d(CGCGAATTCGCG)2 complex of the minor groove binding alkylating agent alkamin studied by mass spectrometry

scientific article published on 24 January 2007

Structure-Activity Relationships for the Anaesthetic and Analgaesic Properties of Aromatic Ring-Substituted Ketamine Esters

scientific article published on 26 June 2020

Structure-activity relationships for 2-anilino-6-phenylpyrido[2,3-d]pyrimidin-7(8H)-ones as inhibitors of the cellular checkpoint kinase Wee1.

scientific article

Structure-activity relationships for 4-nitrobenzyl carbamates of 5-aminobenz[e]indoline minor groove alkylating agents as prodrugs for GDEPT in conjunction with E. coli nitroreductase

scientific article published on June 2003

Structure-activity relationships for amide-, carbamate-, and urea-linked analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824).

scientific article published on 29 December 2011

Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles

scientific article published on 20 February 2018

Structure-activity relationships for analogues of the phenazine-based dual topoisomerase I/II inhibitor XR11576.

scientific article published in February 2002

Structure-activity relationships for pyrido-, imidazo-, pyrazolo-, pyrazino-, and pyrrolophenazinecarboxamides as topoisomerase-targeted anticancer agents

scientific article published in January 2002

Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline

scientific article published on 15 February 2019

Structure-activity relationships of 1,2,4-benzotriazine 1,4-dioxides as hypoxia-selective analogues of tirapazamine

scientific article

Structures and dynamics of DNA complexes of the desmethyl analog of the cytotoxin MLN944: Insights into activity when a methyl isn't futile

scientific article published on 06 April 2020

Structures of two minor-groove-binding quinolinium quaternary salts complexed with d(CGCGAATTCGCG)(2) at 1.6 and 1.8 Angstrom resolution

scientific article

Structure–activity relationships for 4-anilinoquinoline derivatives as inhibitors of the DNA methyltransferase enzyme DNMT1 ⬇️

scientific article published on April 6, 2013

Structure–activity relationships for ketamine esters as short-acting anaesthetics ⬇️

scientific article published on June 27, 2013

Subcellular Location of Tirapazamine Reduction Dramatically Affects Aerobic but Not Anoxic Cytotoxicity

scientific article published on 22 October 2020

Substituted 9-aminoacridine-4-carboxamides tethered to platinum(II)diamine complexes: chemistry, cytotoxicity and DNA sequence selectivity.

scientific article published on 27 March 2010

Substituted arylsulphonamides as inhibitors of perforin-mediated lysis

scientific article published on 26 May 2017

Synergistic Activity of Nitroimidazole-Oxazolidinone Conjugates against Anaerobic Bacteria

scientific article published on 22 May 2020

Syntheses of 8-quinolinolatocobalt(III) complexes containing cyclen based auxiliary ligands as models for hypoxia-activated prodrugs

scientific article published on 22 November 2010

Syntheses, crystal structure and cytotoxicity of diamine platinum(II) complexes containing maltol

scientific article

Synthesis and Evaluation of Imidazo[1,2-a]pyridine Analogues of the ZSTK474 Class of Phosphatidylinositol 3-Kinase Inhibitors

scientific article published on 12 March 2019

Synthesis and Microtubule Destabilizing Activity of N-Cyclopropyl-4-((3,4-dihydroquinolin-1(2H)-yl)sulfonyl)benzamide and its Analogs

scientific article published on 14 November 2018

Synthesis and Structure−Activity Relationships of Aza- and Diazabiphenyl Analogues of the Antitubercular Drug (6S)-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824)

article

Synthesis and anti-inflammatory structure-activity relationships of thiazine-quinoline-quinones: inhibitors of the neutrophil respiratory burst in a model of acute gouty arthritis.

scientific article published on 20 September 2008

Synthesis and biological evaluation of novel analogues of the pan class I phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474).

scientific article

Synthesis and biological evaluation of novel phosphatidylinositol 3-kinase inhibitors: Solubilized 4-substituted benzimidazole analogs of 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474) ⬇️

scientific article published on April 6, 2013

Synthesis and biological evaluation of solubilized sulfonamide analogues of the phosphatidylinositol 3-kinase inhibitor ZSTK474

scientific article published on 25 February 2019

Synthesis and biological evaluation of sulfonamide analogues of the phosphatidylinositol 3-kinase inhibitor ZSTK474.

scientific article published on 20 September 2017

Synthesis and cytotoxic activity of N-(2-diethylamino)ethylcarboxamide and other derivatives of 10H-quindoline

scientific article published in July 2002

Synthesis and cytotoxic activity of N-[(alkylamino)alkyl]carboxamide derivatives of 7-oxo-7H-benz[de]anthracene, 7-oxo-7H-naphtho[1,2,3-de]quinoline, and 7-oxo-7H-benzo[e]perimidine.

scientific article

Synthesis and cytotoxic activity of carboxamide derivatives of benzo[b][1,6]naphthyridin-(5H)ones.

scientific article published on February 2005

Synthesis and cytotoxic activity of carboxamide derivatives of benzo[b][1,6]naphthyridines

scientific article published in March 2003

Synthesis and cytotoxicity of thieno[2,3-b]quinoline-2-carboxamide and cycloalkyl[b]thieno[3,2-e]pyridine-2-carboxamide derivatives.

scientific article published on 27 January 2016

Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units.

scientific article published on 20 October 2017

Synthesis and evaluation of nitroheterocyclic carbamate prodrugs for use with nitroreductase-mediated gene-directed enzyme prodrug therapy

scientific article published on December 2003

Synthesis and evaluation of stable bidentate transition metal complexes of 1-(chloromethyl)-5-hydroxy-3-(5,6,7-trimethoxyindol-2-ylcarbonyl)-2,3-dihydro-1H-pyrrolo[3,2-f]quinoline (seco-6-azaCBI-TMI) as hypoxia selective cytotoxins.

scientific article published on November 2009

Synthesis and evaluation of unsymmetrical bis(arylcarboxamides) designed as topoisomerase-Targeted anticancer drugs ⬇️

scientific article published on 01 January 2002

Synthesis and in vitro evaluation of analogues of avocado-produced toxin (+)-(R)-persin in human breast cancer cells

scientific article

Synthesis and structure-activity relationships for 1-(4-(piperidin-1-ylsulfonyl)phenyl)pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase enzyme AKR1C3

scientific article

Synthesis and structure-activity relationships for 2,4-dinitrobenzamide-5-mustards as prodrugs for the Escherichia coli nfsB nitroreductase in gene therapy

scientific article published on 28 February 2007

Synthesis and structure-activity relationships for extended side chain analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824).

scientific article published on 27 March 2015

Synthesis and structure-activity relationships for tetrahydroisoquinoline-based inhibitors of Mycobacterium tuberculosis

scientific article published on 24 September 2020

Synthesis and structure-activity relationships of N-6 substituted analogues of 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of Wee1 and Chk1 checkpoint kinases

scientific article

Synthesis and structure-activity relationships of antitubercular 2-nitroimidazooxazines bearing heterocyclic side chains

scientific article published in January 2010

Synthesis and structure-activity relationships of soluble 7-substituted 3-(3,5-dimethoxyphenyl)-1,6-naphthyridin-2-amines and related ureas as dual inhibitors of the fibroblast growth factor receptor-1 and vascular endothelial growth factor receptor

scientific article published on July 2005

Synthesis and structure-activity relationships of soluble 8-substituted 4-(2-chlorophenyl)-9-hydroxypyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of the Wee1 and Chk1 checkpoint kinases

scientific article

Synthesis and structure-activity relationships of varied ether linker analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5h-imidazo[2,1-b][1,3]oxazine (PA-824).

scientific article published on September 2011

Synthesis and structure-activity studies of biphenyl analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824).

scientific article published in January 2010

Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110alpha inhibitors.

scientific article published on 4 September 2007

Synthesis, reduction potentials, and antitubercular activity of ring A/B analogues of the bioreductive drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824).

scientific article

Synthetic Studies to Help Elucidate the Metabolism of the Preclinical Candidate TBAJ-876-A Less Toxic and More Potent Analogue of Bedaquiline

scientific article published on 20 March 2020

Synthetic studies utilizing podocarpic acid ⬇️

1969 doctoral thesis by William Alexander Denny at University of Auckland

Systemic and Brain Pharmacokinetics of Perforin Inhibitor Prodrugs

scientific article published on 6 June 2016

Targeting GLUT1 and the Warburg Effect in Renal Cell Carcinoma by Chemical Synthetic Lethality ⬇️

scientific article published on August 3, 2011

Targeting of nanoparticles in cancer: drug delivery and diagnostics

scientific article

Targeting the Warburg Effect in cancer; relationships for 2-arylpyridazinones as inhibitors of the key glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3).

scientific article

The Activity of SN33638, an Inhibitor of AKR1C3, on Testosterone and 17β-Estradiol Production and Function in Castration-Resistant Prostate Cancer and ER-Positive Breast Cancer

scientific article

The DNA sequence selectivity of maltolato-containing cisplatin analogues in purified plasmid DNA and in intact human cells

scientific article published on 13 June 2009

The Nitroimidazooxazines (PA-824 and Analogs): Structure–Activity Relationship and Mechanistic Studies ⬇️

scientific article published on August 1, 2010

The drug vehicle and solvent N-methylpyrrolidone is an immunomodulator and antimyeloma compound

scientific article

The effect of DNA-alkylating agents on gene expression from two integrated reporter genes in a mouse mammary tumor line

scientific article published in March 2002

The effect of a bromide leaving group on the properties of nitro analogs of the duocarmycins as hypoxia-activated prodrugs and phosphate pre-prodrugs for antitumor therapy

scientific article published on 25 August 2011

The effect of sulfonate leaving groups on the hypoxia-selective toxicity of nitro analogs of the duocarmycins

scientific article published on 29 June 2011

The post-lockdown period should be used to acquire effective therapies for future resurgence in SARS-Cov-2 infections

scientific article published on 24 April 2020

The solution structure of bis(phenazine-1-carboxamide)-DNA complexes: MLN 944 binding corrected and extended

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The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents

scientific article published on 02 February 2007

The synthesis of a novel Crizotinib heptamethine cyanine dye conjugate that potentiates the cytostatic and cytotoxic effects of Crizotinib in patient-derived glioblastoma cell lines

scientific article published on 29 July 2019

Therapeutic reactivation of mutant p53 protein by quinazoline derivatives ⬇️

scientific article published on September 13, 2011

Transcription factors as targets for DNA-interacting drugs.

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Transcriptional changes in response to ketamine ester-analogs SN 35210 and SN 35563 in the rat brain

scientific article published on 11 April 2019

Tricyclic [1,2,4]triazine 1,4-dioxides as hypoxia selective cytotoxins

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Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family

scientific article published on 4 August 2016

Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors

scientific article published on February 2006

Unsymmetrical DNA cross-linking agents: combination of the CBI and PBD pharmacophores.

scientific article published on May 2003

Use of three-dimensional tissue cultures to model extravascular transport and predict in vivo activity of hypoxia-targeted anticancer drugs

scientific article published on 01 August 2006

Validating TDP1 as an Inhibition Target for the Development of Chemosensitizers for Camptothecin-Based Chemotherapy Drugs

scientific article published on 23 June 2021

Validation of inhibitors of an ABC transporter required to transport lipopolysaccharide to the cell surface in Escherichia coli ⬇️

scientific article published on April 18, 2013

Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology

scientific article published on 26 November 2019

Weight loss effects of quaternary salts of 5-amino-1-(chloromethyl)-1,2-dihydro-3H-benz[e]indoles; structure–activity relationships ⬇️

scientific article published on December 10, 2011

α₁-Adrenoceptor and serotonin 5-HT(1A) receptor affinity of homobivalent 4-aminoquinoline compounds: an investigation of the effect of linker length

scientific article

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