Potent Antitubulin Tumor Cell Cytotoxins Based on 3-Aroyl Indazoles

A series of 3-aroyl indazoles was synthesized. Modification of the C-7 position resulted in a significant structure−activity relationship (SAR) with acetylene modifications conferring unusual potency in a tumor cell cytotoxicity assay. The most potent compounds exceeded the activity of combretastati...

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Veröffentlicht in:	Journal of medicinal chemistry 2007-03, Vol.50 (5), p.1001-1006
Hauptverfasser:	Duan, Jian-Xin, Cai, Xiaohong, Meng, Fanying, Lan, Leslie, Hart, Charles, Matteucci, Mark
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetylene - chemistry Animals Antineoplastic agents Binding Sites Binding, Competitive Biological and medical sciences Cattle Cell Line, Tumor Colchicine - chemistry Drug Resistance, Neoplasm Drug Screening Assays, Antitumor General aspects Humans Indazoles - chemical synthesis Indazoles - chemistry Indazoles - pharmacology Medical sciences Pharmacology. Drug treatments Radioligand Assay Stilbenes - chemistry Stilbenes - pharmacology Structure-Activity Relationship Tubulin - chemistry Tubulin Modulators - chemical synthesis Tubulin Modulators - chemistry Tubulin Modulators - pharmacology
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