Literature DB >> 15109649

Estrogen receptor ligands. Part 3: The SAR of dihydrobenzoxathiin SERMs.

Helen Y Chen1, Seongkon Kim, Jane Y Wu, Elizabeth T Birzin, Wanda Chan, Yi Tien Yang, Johanna Dahllund, Frank DiNinno, Susan P Rohrer, James M Schaeffer, Milton L Hammond.   

Abstract

A series of 3-alkyl, 3-cycloalkyl, and 3-heteroaryl dihydrobenzoxathiin analogs 1 were prepared and evaluated for estrogen/anti-estrogen activity in both in vitro and in vivo models. In general, the compounds were found to exhibit a high degree of selectivity for ER alpha over ER beta, but were less potent than the original lead compound 1a in the inhibition of estradiol-driven uterine proliferation.

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Year:  2004        PMID: 15109649     DOI: 10.1016/j.bmcl.2004.02.084

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


  3 in total

1.  Prediction of binding affinity for estrogen receptor alpha modulators using statistical learning approaches.

Authors:  Yonghua Wang; Yan Li; Jun Ding; Yuan Wang; Yaqing Chang
Journal:  Mol Divers       Date:  2008-07-26       Impact factor: 2.943

Review 2.  Versatility or promiscuity: the estrogen receptors, control of ligand selectivity and an update on subtype selective ligands.

Authors:  Hui Wen Ng; Roger Perkins; Weida Tong; Huixiao Hong
Journal:  Int J Environ Res Public Health       Date:  2014-08-26       Impact factor: 3.390

3.  1,2-Diaryl(3-pyridyl)ethanone oximes. Intermolecular hydrogen bonding networks revealed by X-ray diffraction.

Authors:  Ermitas Alcalde; Neus Mesquida; Carmen Alvarez-Rúa; Rosa Cuberes; Jordi Frigola; Santiago García-Granda
Journal:  Molecules       Date:  2008-02-07       Impact factor: 4.411

  3 in total

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