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Antitumor agents. Part 202: novel 2'-amino chalcones: design, synthesis and biological evaluation
1Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill 27599, USA.
Bioorganic & Medicinal Chemistry Letters
|April 27, 2000
Abstract:
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.