Antitumor agents. 250. Design and synthesis of new curcumin analogues as potential anti-prostate cancer agents
Antitumor agents. 250. Design and synthesis of new curcumin analogues as potential anti-prostate cancer agents
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DOI：
10.1021/jm051043z
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发表时间：
2006-06-29
影响因子：
7.3
通讯作者：
Lee, Kuo-Hsiung
中科院分区：
文献类型：
--
作者：
Lin, Li;Shi, Qian;Lee, Kuo-Hsiung
In a continuing study of curcumin analogues as potential drug candidates to treat prostate cancer at both androgen-dependent and androgen-refractory stages, we designed and synthesized over 40 new analogues classified into four series: monophenyl analogues ( series A), heterocycle-containing analogues ( series B), analogues bearing various substituents on the phenyl rings ( series C), and analogues with various linkers ( series D). These new compounds were tested for cytotoxicity against two human prostate cancer cell lines, androgen-dependent LNCaP and androgen-independent PC-3. Antiandrogenic activity was also evaluated in LNCaP cells and PC-3 cells transfected with wild-type androgen receptor. Ten compounds possessed potent cytotoxicity against both LNCaP and PC-3 cells, seven only against LNCaP, and one solely against PC-3. This study established an advanced structure-activity relationship ( SAR), and these correlations will guide the further design of new curcumin analogues with better anti-prostate cancer activity.
