Biological evaluation of synthetic analogues of curcumin: chloro-substituted-2′-hydroxychalcones as potential inhibitors of tubulin polymerization and cell proliferation

A series of chloro-substituted-2′-hydroxychalcones were prepared and evaluated for their cytotoxic effects against K562 and SK-N-MC human cancer cell lines and as the inhibitors of tubulin polymerization. The 3,5′-dichloro- analogue (compound 3) inhibited the assembly of protofilaments with 89% inhibition. Compound 3 was found to be bound to tubulin with a dissociation constant of 3.7 μM and altered far-UV circular dichroism spectrum of tubulin and altered far-UV circular dichroism spectrum of tubulin.