Literature DB >> 19356928

Biphenyl C-cyclopropylalkylamides: New scaffolds for targeting estrogen receptor beta.

Miranda J Sarachine1, Jelena M Janjic, Peter Wipf, Billy W Day.   

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)alpha. Further screening of this library identified an ERbeta 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.

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Year:  2009        PMID: 19356928      PMCID: PMC2676897          DOI: 10.1016/j.bmcl.2009.03.075

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  23 in total

1.  Structure of the ligand-binding domain of oestrogen receptor beta in the presence of a partial agonist and a full antagonist.

Authors:  A C Pike; A M Brzozowski; R E Hubbard; T Bonn; A G Thorsell; O Engström; J Ljunggren; J A Gustafsson; M Carlquist
Journal:  EMBO J       Date:  1999-09-01       Impact factor: 11.598

Review 2.  c-Myc in breast cancer.

Authors:  D J Liao; R B Dickson
Journal:  Endocr Relat Cancer       Date:  2000-09       Impact factor: 5.678

3.  Indazole estrogens: highly selective ligands for the estrogen receptor beta.

Authors:  Meri De Angelis; Fabio Stossi; Kathryn A Carlson; Benita S Katzenellenbogen; John A Katzenellenbogen
Journal:  J Med Chem       Date:  2005-02-24       Impact factor: 7.446

4.  Genotoxicity of several clinically used topoisomerase II inhibitors.

Authors:  G Boos; H Stopper
Journal:  Toxicol Lett       Date:  2000-07-27       Impact factor: 4.372

5.  Estrogen receptor beta (ERbeta) and inhibition of prostate cancer cell proliferation: studies on the possible mechanism of action in DU145 cells.

Authors:  A Pravettoni; O Mornati; P G V Martini; M Marino; A Colciago; F Celotti; M Motta; P Negri-Cesi
Journal:  Mol Cell Endocrinol       Date:  2006-10-04       Impact factor: 4.102

6.  Estrogen receptor beta inhibits angiogenesis and growth of T47D breast cancer xenografts.

Authors:  Johan Hartman; Karolina Lindberg; Andrea Morani; José Inzunza; Anders Ström; Jan-Ake Gustafsson
Journal:  Cancer Res       Date:  2006-12-01       Impact factor: 12.701

7.  Microwave-assisted "libraries from libraries" approach toward the synthesis of allyl- and C-cyclopropylalkylamides.

Authors:  Peter Wipf; Claire M Coleman; Jelena M Janjic; Pravin S Iyer; Matthew D Fodor; Yvonne A Shafer; Corey R J Stephenson; Christopher Kendall; Billy W Day
Journal:  J Comb Chem       Date:  2005 Mar-Apr

8.  New antiestrogens from a library screen of homoallylic amides, allylic amides, and C-cyclopropylalkylamides.

Authors:  Jelena M Janjic; Ying Mu; Christopher Kendall; Corey R J Stephenson; Raghavan Balachandran; Brianne S Raccor; Ying Lu; Guangyu Zhu; Wen Xie; Peter Wipf; Billy W Day
Journal:  Bioorg Med Chem       Date:  2005-01-03       Impact factor: 3.641

9.  Expression and role of estrogen receptor alpha and beta in medullary thyroid carcinoma: different roles in cancer growth and apoptosis.

Authors:  Mi Ae Cho; Mi Kyung Lee; Kee-Hyun Nam; Woung Youn Chung; Cheong Soo Park; Ju Hyeong Lee; Taewoong Noh; Woo Ick Yang; Yumie Rhee; Sung-Kil Lim; Hyun Chul Lee; Eun Jig Lee
Journal:  J Endocrinol       Date:  2007-11       Impact factor: 4.286

10.  Estrogen receptor subtypes in ovarian cancer: a clinical correlation.

Authors:  Karen K L Chan; Na Wei; Stephanie S Liu; Liao Xiao-Yun; Annie N Cheung; Hextan Y S Ngan
Journal:  Obstet Gynecol       Date:  2008-01       Impact factor: 7.661

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  1 in total

Review 1.  Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2009.

Authors:  Roland E Dolle; Bertrand Le Bourdonnec; Karin Worm; Guillermo A Morales; Craig J Thomas; Wei Zhang
Journal:  J Comb Chem       Date:  2010-10-05
  1 in total

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