Antitumor agents 290. Design, synthesis, and biological evaluation of new LNCaP and PC-3 cytotoxic curcumin analogs conjugated with anti-androgens

…, E Ohkoshi, L Lin, R Huang, SL Morris-Natschke…

Index: Shi, Qian; Wada, Koji; Ohkoshi, Emika; Lin, Li; Huang, Rong; Morris-Natschke, Susan L.; Goto, Masuo; Lee, Kuo-Hsiung Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 13 p. 4020 - 4031

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Citation Number: 21

Abstract

In our continuing study of curcumin analogs as potential anti-prostate cancer drug candidates, 15 new curcumin analogs were designed, synthesized and evaluated for cytotoxicity against two human prostate cancer cell lines, androgen-dependent LNCaP and androgen-independent PC-3. Twelve analogs (5–12, 15, 16, 19, and 20) are conjugates of curcumin (1) or methyl curcumin (2) with a flutamide-or bicalutamide-like moiety. Two ...