Antitumor agents. Part 202: Novel 2′-amino chalcones: design, synthesis and biological evaluation

New 4′,5′,2,3,4-substituted 2′-amino chalcones were synthesized and evaluated for cytotoxicity against a panel of human tumor cell lines. Several compounds displayed significant cytotoxicity. The most promising lead molecule (10) also had high activity toward multi-drug resistant KB-VIN, and ovarian 1A9 cell lines. 2′-Amino chalcones demonstrated significantly increased antitumor activity compared with the corresponding chalcones, while, the epoxide derivatives generally showed greatly reduced activity. Scheme 1. General synthetic routes to 2′-amino chalcones.