Molecular modifications of 2-arylidene-1-indanones leading to increased cytotoxic potencies

作者:Pati Hari N; Das Umashankar; De Clercq Erik; Balzarini Jan; Dimmock Jonathan R*
来源:Journal of Enzyme Inhibition and Medicinal Chemistry, 2007, 22(1): 37-42.
DOI:10.1080/14756360600958057

摘要

A series of 2-arylidene-1-indanones, 1, had been shown previously to display cytotoxic properties towards Molt 4/C8, CEM and L1210 cells. In the present study, two series of analogues of 1 were prepared namely various 2-arylidene- 1,3-indandiones, 2, and chalcones, 3. In general, the potencies of compounds 2 and 3 were greater than the analogues bearing the same aryl substituents in series 1. Molecular modeling was undertaken in order to seek explanations for the variation in bioactivities.