Synthesis and cytotoxicity of epoxide and pyrazole analogs of the combretastatins

…, M Stewart, HN Pati, D VanDerveer, H Arman…

Index: LeBlanc, Regan; Dickson, John; Brown, Toni; Stewart, Michelle; Pati, Hari N.; VanDerveer, Don; Arman, Hadi; Harris, Jeff; Pennington, William; Holt Jr., Herman L.; Lee, Moses Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 21 p. 6025 - 6034

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Citation Number: 89

Abstract

Twenty-six epoxide and corresponding pyrazole derivatives, of the structurally related chalcones and combretastatin A-4 (CA-4), were synthesized and tested for in vitro cytotoxicity. These molecules were synthesized by epoxidation of the relevant chalcones, followed by reaction with hydrazine. The structures of epoxides 3 and 7, and pyrazole 17, were confirmed by X-ray diffraction studies. The relatively coplanar conformation of a 3′, ...