Structure-activity relationships for a family of benzothiophene selective estrogen receptor modulators including raloxifene and arzoxifene.

Structure-activity relationships for a family of benzothiophene selective estrogen receptor modulators including raloxifene and arzoxifene. Research Abstract Details 

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Structure-activity relationships for a family of benzothiophene selective estrogen receptor modulators including raloxifene and arzoxifene. Abstract Text:

Cassia R Overk,Kuan-Wei Peng,Rezene T Asghodom,Irida Kastrati,Daniel D Lantvit,Zhihui Qin,Jonna Frasor,Judy L Bolton,Gregory R J Thatcher,

The search for the "ideal" selective estrogen receptor modulator (SERM) as a substitute for hormone replacement therapy (HRT) or use in cancer chemoprevention has focused on optimization of estrogen receptor (ER) ligand binding. Based on the clinical and preclinical benzothiophene SERMs, raloxifene and arzoxifene, a family of SERMs has been developed to modulate activity and oxidative lability. Antiestrogenic potency measured in human endometrial and breast cancer cells, and ER ligand binding data were correlated and seen to provide a guide to SERM design only when viewed in toto. The in vitro studies were extended to the juvenile rat model, in which the desired antiestrogenic profile and putative cardiovascular benefits of SERMs were observed.

Structure-activity relationships for a family of benzothiophene selective estrogen receptor modulators including raloxifene and arzoxifene. Publishing Authors By Initials

CR Overk,KW Peng,RT Asghodom,I Kastrati,DD Lantvit,Z Qin,J Frasor,JL Bolton,GR Thatcher,

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Structure-activity relationships for a family of benzothiophene selective estrogen receptor modulators including raloxifene and arzoxifene. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: ChemMedChem

VOLUME: 2

Page Numbers: 1520-6

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ISSN: 1860-7179

DAY: 1

MONTH: Oct

YEAR: 2007

Structure-activity relationships for a family of benzothiophene selective estrogen receptor modulators including raloxifene and arzoxifene. Information

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LANGUAGE: eng

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AFFILIATION: Department of Medicinal Chemistry & Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 S Wood St, Chicago, IL, 60612, USA, Fax: (+1) 312-996-7107.

Country: Germany

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MEDLINETA: ChemMedChem

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