Synthesis and biological evaluation of new disubstituted analogues of 6-methoxy-3-(3′, 4′, 5′-trimethoxybenzoyl)-1H-indole (BPR0L075), as potential antivascular …

…, G Dupeyre, GG Chabot, J Seguin, F Tillequin…

Index: Ty, Nancy; Dupeyre, Gregory; Chabot, Guy G.; Seguin, Johanne; Tillequin, Francois; Scherman, Daniel; Michel, Sylvie; Cachet, Xavier Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 15 p. 7494 - 7503

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Citation Number: 26

Abstract

6-Methoxy-3-(3′, 4′, 5′-trimethoxybenzoyl)-1H-indole (BPR0L075)(1) is a potent inhibitor of tubulin polymerization which exhibits both in vitro and in vivo activities against a broad spectrum of solid tumors. This compound was designed as a heterocyclic analogue of combretastatin A4 (CA-4), a natural stilbene derivative that disrupts the tumor vasculature and causes tumor regression. In the present work, we describe the design and synthesis ...