A boronic acid chalcone analog of combretastatin A-4 as a potent anti-proliferation agent

…, E Hamel, SL Mooberry, MA Paige, ML Brown

Index: Kong, Yali; Wang, Kan; Edler, Michael C.; Hamel, Ernest; Mooberry, Susan L.; Paige, Mikell A.; Brown, Milton L. Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 2 p. 971 - 977

Full Text: HTML

Citation Number: 64

Abstract

Chalcones represent a class of natural products that inhibits tubulin assembly. In this study we designed and synthesized boronic acid analogs of chalcones in an effort to compare biological activities with combretastatin A-4, a potent inhibitor of tubulin polymerization. Systematic evaluation of the positional effects of the carbonyl moiety towards inhibition of tubulin polymerization, cancer cell proliferation and angiogenesis revealed that placement ...