Targeting the estrogen receptor with metal-carbonyl derivatives of estradiol.
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ABSTRACT:
SUBMITTER: Hanson RN
PROVIDER: S-EPMC3274643 | biostudies-literature | 2012 Feb
REPOSITORIES: biostudies-literature
Publications
Targeting the estrogen receptor with metal-carbonyl derivatives of estradiol.
Hanson Robert N RN Kirss Rein R McCaskill Emmett E Hua Edward E Tongcharoensirikul Pakamas P Olmsted Sandra L SL Labaree David D Hochberg Richard B RB
Bioorganic & medicinal chemistry letters 20120108 4
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 compar ...[more]
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