Search Results - "DREWE, John"
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Discovery of 4-aryl-4H-chromenes as potent apoptosis inducers using a cell- and caspase-based Anti-cancer Screening Apoptosis Program (ASAP): SAR studies and the identification of novel vascular disrupting agents
Published in Anti-cancer agents in medicinal chemistry (01-05-2009)“…Many cancer cells are known to have defects in the apoptosis machinery. Therefore identification of compounds that can activate or promote apoptosis in cancer…”
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Discovery of 4-Aryl-4H-chromenes as a New Series of Apoptosis Inducers Using a Cell- and Caspase-Based High Throughput Screening Assay. 4. Structure–Activity Relationships of N-Alkyl Substituted Pyrrole Fused at the 7,8-Positions
Published in Journal of medicinal chemistry (14-02-2008)“…In our continuing effort to discover and develop apoptosis inducing 4-aryl-4H-chromenes as novel anticancer agents, we explored the structure−activity…”
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Discovery and Structure−Activity Relationship of 3-Aryl-5-aryl-1,2,4-oxadiazoles as a New Series of Apoptosis Inducers and Potential Anticancer Agents
Published in Journal of medicinal chemistry (11-08-2005)“…We have identified 5-(3-chlorothiophen-2-yl)-3-(4-trifluoromethylphenyl)-1,2,4-oxadiazole (1d) as a novel apoptosis inducer through our caspase- and cell-based…”
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A chemical genetics approach for the discovery of apoptosis inducers: from phenotypic cell based HTS assay and structure-activity relationship studies, to identification of potential anticancer agents and molecular targets
Published in Current medicinal chemistry (01-09-2006)“…The approach of chemical genetics has been widely used to study biological systems and to discover new drugs, signaling pathways and targets. The current…”
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Antivascular and antitumor evaluation of 2-amino-4-(3-bromo-4,5-dimethoxy-phenyl)-3-cyano-4H-chromenes, a novel series of anticancer agents
Published in Molecular cancer therapeutics (01-11-2004)“…A novel series of 2-amino-4-(3-bromo-4,5-dimethoxy-phenyl)-3-cyano-4 H -chromenes was identified as potent apoptosis inducers through a cell-based high…”
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Discovery, characterization and SAR of gambogic acid as a potent apoptosis inducer by a HTS assay
Published in Bioorganic & medicinal chemistry (15-01-2004)“…Gambogic acid (2), a natural product isolated from the resin of Garcinia hurburyi tree, was discovered to be a potent apoptosis inducer using our cell- and…”
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Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2. Structure-activity relationships of the 7- and 5-, 6-, 8-positions
Published in Bioorganic & medicinal chemistry letters (01-11-2005)“…As a continuation of our efforts to discover and develop the apoptosis inducing 4-aryl-4H-chromenes as novel anticancer agents, we explored the SAR of…”
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A Role for Transferrin Receptor in Triggering Apoptosis When Targeted with Gambogic Acid
Published in Proceedings of the National Academy of Sciences - PNAS (23-08-2005)“…Transferrin receptor (TfR) has been shown to be significantly overexpressed in different types of cancers. We discovered TfR as a target for gambogic acid…”
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Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell-and caspase-based HTS assay. Part 5: Modifications of the 2-and 3-positions
Published in Bioorganic & medicinal chemistry (15-01-2008)“…As a continuation of our efforts to discover and develop apoptosis inducing 4-aryl-4H-chromenes as novel anticancer agents, we explored modifications at the 2-…”
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Discovery of 4-anilino- N-methylthieno[3,2- d]pyrimidines and 4-anilino- N-methylthieno[2,3- d]pyrimidines as potent apoptosis inducers
Published in Bioorganic & medicinal chemistry letters (01-07-2009)“…The discovery and SAR studies of 4-anilino -N-methylthieno[3,2- d]pyrimidines and 4-anilino -N-methylthieno[2,3- d]pyrimidines as potent apoptosis inducers are…”
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Discovery of 1-benzoyl-3-cyanopyrrolo[1,2-a]quinolines as a new series of apoptosis inducers using a cell-and caspase-based high-throughput screening assay. Part 1: Structure-activity relationships of the 1-and 3-positions
Published in Bioorganic & medicinal chemistry letters (01-12-2008)“…1-Benzoyl-3-cyanopyrrolo[1,2-a]quinoline (2a) was identified as a novel apoptosis inducer through our caspase- and cell-based high-throughput screening assay…”
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Discovery and mechanism of action of a novel series of apoptosis inducers with potential vascular targeting activity
Published in Molecular cancer therapeutics (01-11-2004)“…A novel series of 2-amino-4-(3-bromo-4,5-dimethoxy-phenyl)-3-cyano-4 H -chromenes was identified as apoptosis-inducing agents through our cell-based apoptosis…”
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Selective activation of apoptosis by a novel set of 4-aryl-3-(3-aryl-1-oxo-2-propenyl)-2( 1H )-quinolinones through a Myc-dependent pathway
Published in Cancer letters (18-02-2009)“…Abstract Oncogene addiction due to Myc deregulation has been identified in a variety of tumor types. In order to identify pharmacological agents that cause…”
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Discovery of substituted N′-(2-oxoindolin-3-ylidene)benzohydrazides as new apoptosis inducers using a cell- and caspase-based HTS assay
Published in Bioorganic & medicinal chemistry letters (15-05-2009)“…The discovery and SAR studies of substituted N′-(2-oxoindolin-3-ylidene)benzohydrazides as novel and potent apoptosis inducers are reported. We report the…”
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Discovery of N-methyl-4-(4-methoxyanilino)quinazolines as potent apoptosis inducers. Structure–activity relationship of the quinazoline ring
Published in Bioorganic & medicinal chemistry letters (01-04-2010)“…The synthesis and SAR studies of the quinazoline ring of N-methyl-4-(4-methoxyanilino)quinazolines as novel apoptosis inducers are reported. As a continuation…”
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Discovery and SAR of indole-2-carboxylic acid benzylidene-hydrazides as a new series of potent apoptosis inducers using a cell-based HTS assay
Published in Bioorganic & medicinal chemistry (01-07-2004)“…The discovery of indole-2-carboxylic acid benzylidene-hydrazides as a new series of potent inducers of apoptosis using a cell- and caspase-based HTS assay, as…”
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Discovery of Substituted N-Phenyl Nicotinamides as Potent Inducers of Apoptosis Using a Cell- and Caspase-Based High Throughput Screening Assay
Published in Journal of medicinal chemistry (05-06-2003)“…By applying a novel cell- and caspase-based HTS assay, a series of N-phenyl nicotinamides has been identified as a new class of potent inducers of apoptosis…”
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The discovery and mechanism of action of novel tumor-selective and apoptosis-inducing 3,5-diaryl-1,2,4-oxadiazole series using a chemical genetics approach
Published in Molecular cancer therapeutics (01-05-2005)“…A novel series of 3,5-diaryl-oxadiazoles was identified as apoptosis-inducing agents through our cell and chemical genetics–based screening assay for compounds…”
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Exchange of Conduction Pathways Between Two Related K$^+$ Channels
Published in Science (American Association for the Advancement of Science) (22-02-1991)“…The structure of the ion conduction pathway or pore of voltage-gated ion channels is unknown, although the linker between the membrane spanning segments S5 and…”
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[3H]Ethynylbicycloorthobenzoate ([3H]EBOB) binding in recombinant GABAA receptors
Published in Neurotoxicology (Park Forest South) (01-12-2003)“…Ethynylbicycloorthobenzoate (EBOB) is a recently developed ligand that binds to the convulsant site of the GABAA receptor. While a few studies have examined…”
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