Targeting the estrogen receptor with metal-carbonyl derivatives of estradiol.

Targeting the estrogen receptor with metal-carbonyl derivatives of estradiol.
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DOI:
10.1016/j.bmcl.2011.12.111
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发表时间:
2012-02-15
影响因子:
2.7
通讯作者:
Hochberg, Richard B.
Hochberg, Richard B.
中科院分区:
医学4区
文献类型:
--
作者:
Hanson, Robert N.;Kirss, Rein;McCaskill, Emmett;Hua, Edward;Tongcharoensirikul, Pakamas;Olmsted, Sandra L.;Labaree, David;Hochberg, Richard B.

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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 estadiol analog, but lower than that of the phenyl vinyl estradiol analog.
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