Inhibition of tubulin polymerization is an important approach for cancer therapy. The design of colchicine site ligands has attracted special interest throughout the last years. Work within our group has led to the development of cytotoxic chalcones that are able to inhibit tubulin polymerization in vitro and to provoke cellular mitotic arrest. Considering that the migration of metastatic cancer cells requires remodeling of the cytoskeleton, including the regulation of microtubules, we have evaluated a series of chalcone derivatives for its ability to inhibit cancer cell migration, using the wound healing and Boyden-chamber cell migration assays. Two chalcones inhibited invasive MDA-MB-231 cell migration in a dose-dependent manner similar to that of colchicine (IC50 range 475-1095 nM). Together, these findings represent important advances toward the investigation of the anti-metastatic effects of the developed chalcones. The structure-activity relationships and biological data of this series will be presented and discussed.

Design of 3,4,5-trimethoxychalcones as mitotic arresters and cell migration inhibitors

243rd National Meeting (2012)

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