用雌二醇的金属羰基衍生物靶向雌激素受体。
Targeting the estrogen receptor with metal-carbonyl derivatives of estradiol.
机构信息
Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA 02115-5000, USA.
出版信息
Bioorg Med Chem Lett. 2012 Feb 15;22(4):1670-3. doi: 10.1016/j.bmcl.2011.12.111. Epub 2012 Jan 8.
Abstract
As part of our program to develop new probes for the estrogen receptor binding domain, we prepared and evaluated a novel 17α-(rhenium tricarbonyl bipyridyl) vinyl estradiol complex. Preparation of the final compound was achieved using the Stille coupling between the preformed brominated rhenium tricarbonyl bipyridine complex and the tributylstannyl vinyl estradiol. Competitive receptor binding assays and stimulatory assays demonstrated that the final complex retained affinity and efficacy comparable to the corresponding pyridyl vinyl estradiol analog, but lower than that of the phenyl vinyl estradiol analog.
摘要
作为开发新的雌激素受体结合域探针计划的一部分，我们制备并评估了一种新型的 17α-（铼三羰基联吡啶）乙烯雌二醇配合物。最后化合物的制备是通过预形成的溴化铼三羰基联吡啶配合物与三丁基锡基乙烯雌二醇之间的 Stille 偶联来实现的。竞争性受体结合测定和刺激测定表明，最终的配合物保留了与相应的吡啶基乙烯雌二醇类似物相当的亲和力和效力，但低于苯乙烯雌二醇类似物。
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