金属有机类选择性雌激素受体调节剂(SERMs)研究进展  

Progress in organometallic selective estrogen receptor modulators (SERMs)

作　　者：郑阳钒[1] 周海兵[1] 

机构地区：[1]武汉大学药学院,湖北武汉430071

出　　处：《中国药物化学杂志》2012年第3期236-245,共10页Chinese Journal of Medicinal Chemistry

基　　金：国家自然科学基金项目(20872116)

摘　　要：近年来金属有机化学的研究发展迅速,很多金属有机类化合物常常可以产生常规有机化合物所不具有的一些意外的药效作用,因此,在很多药物分子结构中都引入了金属基团。为了提高乳腺癌的治愈率,世界各地的研究小组把一些活性金属基团引入到一些具有潜在抗乳腺癌活性的分子中,形成了一类独特的金属有机类选择性雌激素受体调节剂(selective estrogen receptor modulators,SERMs),在研究过程中发现多个系列的金属有机类SERMs在脂溶性、与受体的结合力以及抑制乳腺癌细胞增殖等方面都表现出一定的优势。该文对近年来金属有机类SERMs的研究成果进行综述。In recent years,organometallic chemistry has been rapidly developed.Diverse of metals were introduced into various of pharmacophores producing unexpected biological effects compared to traditional organic compounds.In order to enhance the cure rate of the breast cancer,many research groups made efforts to introduce the active organometallic groups into the potential scaffolds to form a special type of selective estrogen receptor modulators,in which many of them exhibited appropriate advantages in lipid solubility,receptor binding affinity and the ability to suppress proliferation of the related breast cancer cells.The progress of this field were discussed in this review.

关 键 词：雌激素受体 乳腺癌 选择性雌激素受体调节剂 金属有机化合物 

分 类 号：R977.1[医药卫生—药品]