| Literature DB >> 16789753 |
Li Lin1, Qian Shi, Alexander K Nyarko, Kenneth F Bastow, Chin-Chung Wu, Ching-Yuan Su, Charles C-Y Shih, Kuo-Hsiung Lee.
Abstract
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.Entities:
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Year: 2006 PMID： 16789753 PMCID： PMC2597393 DOI： 10.1021/jm051043z
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446