Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site.
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DOI: 10.1021/acs.jmedchem.2c01208
Abstract: Targeting the colchicine binding site on tubulin is a promising strategy to develop cancer therapeutics. Herein, we describe our systematic structure-activity relationship studies of benzamide derivatives that lead to an identification of a potent and… read more here.
Keywords: tubulin; benzamide derivatives; colchicine binding; targeting colchicine ... See more keywords
Discovery of Novel 4,5-Dihydropyrrolo[3,4-c]pyrazol-6(2H)-one-Based Tubulin Inhibitors Targeting Colchicine Binding Site with Potent Anti-Ovarian Cancer Activity.
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DOI: 10.1021/acs.jmedchem.5c00014
Abstract: To address the toxicity of current microtubule inhibitors, we employed the GeminiMol deep learning model to screen the Zinc20 database, identifying a novel 4,5-dihydropyrrolo[3,4-c]pyrazol-6(2H)-one scaffold (Y1) targeting the colchicine binding site. Subsequent optimization culminated in… read more here.
Keywords: novel dihydropyrrolo; tubulin; pyrazol one; dihydropyrrolo pyrazol ... See more keywords