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

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

Index: 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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Citation Number: 18

Abstract

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 ...