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Biphenyl C-cyclopropylalkylamides: New scaffolds for targeting estrogen receptor β

Sarachine, MJ and Janjic, JM and Wipf, P and Day, BW (2009) Biphenyl C-cyclopropylalkylamides: New scaffolds for targeting estrogen receptor β. Bioorganic and Medicinal Chemistry Letters, 19 (9). 2404 - 2408. ISSN 0960-894X

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The C-cyclopropylalkylamide scaffold was previously identified as a new structural framework for antiestrogens. A second generation library provided three compounds that bind estrogen receptor (ER)α. Further screening of this library identified an ERβ hit and inspired another round of SAR. A new focused library was tested for binding to the ERs, and for effects on the growth of breast cancer cell lines and protein levels of common cell cycle regulators. © 2009 Elsevier Ltd. All rights reserved.


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Item Type: Article
Status: Published
CreatorsEmailPitt UsernameORCID
Sarachine, MJ
Janjic, JMjmj116@pitt.eduJMJ1160000-0002-0539-8359
Wipf, Ppwipf@pitt.eduPWIPF
Day, BW
Date: 1 May 2009
Date Type: Publication
Journal or Publication Title: Bioorganic and Medicinal Chemistry Letters
Volume: 19
Number: 9
Page Range: 2404 - 2408
DOI or Unique Handle: 10.1016/j.bmcl.2009.03.075
Schools and Programs: Dietrich School of Arts and Sciences > Chemistry
Refereed: Yes
ISSN: 0960-894X
MeSH Headings: Amides--chemical synthesis; Amides--chemistry; Antineoplastic Agents--chemical synthesis; Antineoplastic Agents--pharmacology; Binding, Competitive; Cell Cycle; Cell Line, Tumor; Cell Proliferation--drug effects; Chemistry, Pharmaceutical--methods; Estrogen Receptor beta--chemistry; Humans; Inhibitory Concentration 50; Ligands; Models, Chemical; Protein Binding; Protein Isoforms; Structure-Activity Relationship
Other ID: NLM NIHMS105130, NLM PMC2676897
PubMed Central ID: PMC2676897
PubMed ID: 19356928
Date Deposited: 07 Jun 2013 20:48
Last Modified: 07 Aug 2021 14:55


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