Literature DB >> 3199805

Non-isomerisable antiestrogens related to tamoxifen.

R McCague1, M Jarman, O T Leung, A B Foster, G Leclercq, S Stoessel.   

Abstract

Three types of non-isomerisable antiestrogens analogous to tamoxifen and 4-hydroxytamoxifen are described. Advantages of non-isomerisability are simplified synthesis, simplified metabolism profile, and that structure-activity relationships become more meaningful. The compounds described differ from tamoxifen by having an extra ring methyl group, a fused seven-membered ring system, or the central ethylene linkage saturated. These compounds retained both binding affinity to estrogen receptors and growth inhibition of MCF-7 human breast cancer cells in vitro.

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Year:  1988        PMID: 3199805     DOI: 10.1016/0022-4731(88)90005-2

Source DB:  PubMed          Journal:  J Steroid Biochem        ISSN: 0022-4731            Impact factor:   4.292


  2 in total

1.  Molecular determinants of tissue selectivity in estrogen receptor modulators.

Authors:  T A Grese; J P Sluka; H U Bryant; G J Cullinan; A L Glasebrook; C D Jones; K Matsumoto; A D Palkowitz; M Sato; J D Termine; M A Winter; N N Yang; J A Dodge
Journal:  Proc Natl Acad Sci U S A       Date:  1997-12-09       Impact factor: 11.205

2.  Design and synthesis of novel selective estrogen receptor degradation inducers based on the diphenylheptane skeleton.

Authors:  Takashi Misawa; Takuma Fujisato; Yasunari Kanda; Nobumichi Ohoka; Takuji Shoda; Momoko Yorioka; Makoto Makishima; Yuko Sekino; Mikihiko Naito; Yosuke Demizu; Masaaki Kurihara
Journal:  Medchemcomm       Date:  2016-12-08       Impact factor: 3.597

  2 in total

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