Anti-cancer agents in medicinal chemistry, 2011, 12(3):271-81.

Genistein and its Synthetic Analogs as Anticancer Agents

Qing-Shan Li, Cui-Yun Li, Zi-Lin Li, et al

State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing, P. R.China

Genistein, one of the predominant isoflavones derived from soybeans, has been shown beneficial effects in cancer prevention and treatment. There is an accumulating body of experimental evidences suggesting that genistein affects cancer progression by increasing apoptosis, inducing cell cycle arrest,modulating intracellular signaling pathways, and inhibiting invasion and metastasis of cancer cells. During last decade, many researchers have conducted extensive studies by synthesizing amounts of structurally-modified derivatives based on the isoflavone skeleton of genistein to enhance its anticancer activity, some analogs of which possess more potent activities of the prevention and/or treatment of various cancers. In this review, we summarized the current knowledge regarding anticancer effects,structure-activity relationships and action mechanisms of genistein and its synthesized analogs, which would be beneficial to the rational design of new genistein derivatives as anticancer drugs.

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荷兰《药物化学中的抗癌药物》，2012年3月

金雀异黄素及其合成类似物作为抗癌药物

李青山，李翠云，李子琳，等

中国南京大学医药生物技术国家重点实验室

金雀异黄素，是一种来源于大豆的主要异黄酮，在预防和治疗癌症方面具有有益的影响。越来越多的实验证据表明，金雀异黄素通过增加细胞凋亡、 诱导细胞周期阻滞、 调节细胞内信号通路，抑制肿瘤细胞的侵袭和转移影响癌症的进展。在过去的十年间，许多研究者进行了广泛研究，基于金雀异黄素的异黄酮骨架合成了结构改性的衍生物，增强其抗癌的活性，其中一些类似物具有更强效的预防和 （或） 治疗各种癌症活性。在本综述中，我们总结了当前关于抗癌作用、 结构-活性关系和金雀异黄素及其合成类似物的活性机制的知识，将有益于合理设计新型金雀异黄素衍生物作为抗癌药物。