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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Abstract
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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Details
Item Type: |
Article
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Status: |
Published |
Creators/Authors: |
Creators | Email | Pitt Username | ORCID |
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Sarachine, MJ | | | | Janjic, JM | | | | Wipf, P | pwipf@pitt.edu | PWIPF | | Day, BW | | | |
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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: |
02 Feb 2019 15:57 |
URI: |
http://d-scholarship-dev.library.pitt.edu/id/eprint/18879 |
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