基于紫罗兰酮的查耳酮的合成及其潜在的抗前列腺癌活性。
Syntheses and potential anti-prostate cancer activities of ionone-based chalcones.
作者信息
Zhou Jinming, Geng Guoyan, Batist Gerald, Wu Jian Hui
机构信息
Department of Oncology, McGill University, Montreal, Canada.
出版信息
Bioorg Med Chem Lett. 2009 Feb 15;19(4):1183-6. doi: 10.1016/j.bmcl.2008.12.089. Epub 2008 Dec 25.
We report the SAR studies of 43 ionone-based chalcones that demonstrate substantial in vitro anti-proliferative activities in LNCaP, MDA-PCa-2b, 22Rv1, C4-2B and PC-3 prostate cancer cell lines. Compound 25 with an IC(50) value of 0.74 microM in LNCaP cells potently antagonizes DHT-induced transactivation of the wild type and the clinically relevant T877A, W741C and H874Y mutated androgen receptors, representing a novel chalcone as pan-antagonist of androgen receptor.
我们报告了43种基于紫罗兰酮的查尔酮的构效关系研究，这些研究表明它们在LNCaP、MDA-PCa-2b、22Rv1、C4-2B和PC-3前列腺癌细胞系中具有显著的体外抗增殖活性。化合物25在LNCaP细胞中的IC(50)值为0.74微摩尔，能有效拮抗双氢睾酮诱导的野生型以及临床相关的T877A、W741C和H874Y突变雄激素受体的反式激活，代表了一种新型的作为雄激素受体泛拮抗剂的查尔酮。
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