A Concise Synthesis of Pyrazole Analogues of Combretastatin A1 as Potent Anti??Tubulin Agents

R Zaninetti, SV Cortese, S Aprile, A Massarotti…

文献索引：Zaninetti, Roberta; Cortese, Salvatore V.; Aprile, Silvio; Massarotti, Alberto; Canonico, Pier Luigi; Sorba, Giovanni; Grosa, Giorgio; Genazzani, Armando A.; Pirali, Tracey ChemMedChem, 2013 , vol. 8, # 4 p. 633 - 643

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被引用次数: 18

摘要

Abstract Combretastatin A1 (CA1) binds to the β-subunit at the colchicine binding site of tubulin and inhibits polymerization. As such, it is both an antitumor agent and a vascular disrupting agent. It has been shown to be at least tenfold more potent than combretastatin A4 (CA4) in terms of vascular shutdown, which correlates with its metabolism to reactive ortho-quinone species that are assumed to be directly cytotoxic in tumor cells. A series of ...