姜黄素类似物的构效关系研究
Structure-activity relationship studies of curcumin analogues.
作者信息
Fuchs James R, Pandit Bulbul, Bhasin Deepak, Etter Jonathan P, Regan Nicholas, Abdelhamid Dalia, Li Chenglong, Lin Jiayuh, Li Pui-Kai
机构信息
Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 338 Parks Hall, 500 West 12th Avenue, Columbus, OH 43210, USA.
出版信息
Bioorg Med Chem Lett. 2009 Apr 1;19(7):2065-9. doi: 10.1016/j.bmcl.2009.01.104. Epub 2009 Feb 5.
Two series of curcumin analogues, a total of twenty-four compounds, were synthesized and evaluated. The most potent compound, compound 23, showed potent growth inhibitory activities on both prostate and breast cancer lines with IC(50) values in sub-micromolar range, fifty times more potent than curcumin. Curcumin analogues might be potential anti-tumor agents for breast and prostate cancers.
合成并评估了两系列姜黄素类似物，共24种化合物。最有效的化合物23对前列腺癌和乳腺癌细胞系均显示出强大的生长抑制活性，其IC(50)值在亚微摩尔范围内，比姜黄素的活性强50倍。姜黄素类似物可能是用于乳腺癌和前列腺癌的潜在抗肿瘤药物。
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