Literature DB >> 12749895

Tetrahydroquinoline-based selective estrogen receptor modulators (SERMs).

Owen B Wallace1, Kenneth S Lauwers, Scott A Jones, Jeffrey A Dodge.   

Abstract

A new series of estrogen receptor ligands based on a 6-hydroxy-tetrahydroquinoline scaffold is described, in addition to their binding affinity and functional activity in MCF-7 cells. Several 1,2-disubstituted tetrahydroquinolines bearing a basic side chain were shown to be high affinity ligands and antagonists in the MCF-7 proliferation assay. Compounds lacking the basic side chain were agonists in the MCF-7 assay.

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Year:  2003        PMID: 12749895     DOI: 10.1016/s0960-894x(03)00306-8

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


  5 in total

1.  Structure‒tissue exposure/selectivity relationship (STR) correlates with clinical efficacy/safety.

Authors:  Wei Gao; Hongxiang Hu; Lipeng Dai; Miao He; Hebao Yuan; Huixia Zhang; Jinhui Liao; Bo Wen; Yan Li; Maria Palmisano; Mohamed Dit Mady Traore; Simon Zhou; Duxin Sun
Journal:  Acta Pharm Sin B       Date:  2022-02-23       Impact factor: 14.903

2.  Quinoline: A versatile heterocyclic.

Authors:  Akranth Marella; Om Prakash Tanwar; Rikta Saha; Mohammad Rahmat Ali; Sandeep Srivastava; Mymoona Akhter; Mohammad Shaquiquzzaman; Mohammad Mumtaz Alam
Journal:  Saudi Pharm J       Date:  2012-03-29       Impact factor: 4.330

3.  Kinetic resolution of racemic 2-substituted 1,2-dihydroquinolines via asymmetric Cu-catalyzed borylation.

Authors:  Duanyang Kong; Suna Han; Rui Wang; Meina Li; Guofu Zi; Guohua Hou
Journal:  Chem Sci       Date:  2017-04-19       Impact factor: 9.825

4.  Construction of azaheterocycles via Pd-catalyzed migratory cycloannulation reaction of unactivated alkenes.

Authors:  Jin-Ping Wang; Shuo Song; Yichen Wu; Peng Wang
Journal:  Nat Commun       Date:  2022-08-27       Impact factor: 17.694

5.  New recombinant cyclohexylamine oxidase variants for deracemization of secondary amines by orthogonally assaying designed mutants with structurally diverse substrates.

Authors:  Guangyue Li; Peiyuan Yao; Peiqian Cong; Jie Ren; Lei Wang; Jinhui Feng; Peter C K Lau; Qiaqing Wu; Dunming Zhu
Journal:  Sci Rep       Date:  2016-05-03       Impact factor: 4.379

  5 in total

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