Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies.

Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies. Research Abstract Details 

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Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies. Abstract Text:

Timothy I Richardson,Jeffrey A Dodge,Yong Wang,Jim D Durbin,Venkatesh Krishnan,Bryan H Norman,Timothy I Richardson,Jeffrey A Dodge,Yong Wang,Jim D Durbin,Venkatesh Krishnan,Bryan H Norman,

Benzopyrans are selective estrogen receptor (ER) beta agonists (SERBAs), which bind the ER subtypes alpha and beta in opposite orientations. Here we describe the synthesis of a late stage intermediate that allowed us to combine A-ring and C-ring modifications and carry out simultaneous SAR studies at both positions. Modification of both positions proved additive, maintaining affinity and improving ERbeta selectivity up to 83-fold. An X-ray cocrystal structure confirms the previously observed binding mode in ERbeta.

Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies. Publishing Authors By Initials

TI Richardson,JA Dodge,Y Wang,JD Durbin,V Krishnan,BH Norman,TI Richardson,JA Dodge,Y Wang,JD Durbin,V Krishnan,BH Norman,

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Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 17

Page Numbers: 5563-6

Journal Abbreviation: Bioorg. Med. Chem. Lett.

ISSN: 0960-894X

DAY: 11

MONTH: 08

YEAR: 2007

Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies. Information

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LANGUAGE: eng

NlmUniqueID: 9107377

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Grant and Affiliation Information for Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies.

AFFILIATION: Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. t_richardson@lilly.com

Country: England

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MEDLINETA: Bioorg Med Chem Lett

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