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Literature DB >> 2815158

Novel steroidal pure antiestrogens.

J Bowler¹, T J Lilley, J D Pittam, A E Wakeling.

Abstract

A series of steroidal estrogen antagonists with no intrinsic estrogenicity in rat uterotrophic-antiuterotrophic tests has been discovered. The compounds are derivatives of estradiol containing amidoalkyl side chains at the 7 alpha-position. The most potent compounds are N-n-butyl-N-methyl-11-(3,17 beta-dihydroxyestra- 1,3,5(10)-trien-7 alpha-yl) undecanamide and N-2,2,3,3,4,4,4-heptafluorobutyl-N-methyl-11-(3,17 beta-dihydroxyestra- 1,3,5(10)-trien-7 alpha-yl) undecanamide. Structure activity relationships are discussed.

Entities: Chemical Species

Mesh：

Substances：
Estrogen Antagonists

Year: 1989 PMID： 2815158 DOI： 10.1016/0039-128x(89)90076-7

Source DB: PubMed Journal: Steroids ISSN： 0039-128X Impact factor: 2.668

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Cited

24 in total

1. New chemical syntheses of cholest-4,6-dien-3-one.

Authors: Edward J Parish; Hang Sun; Ding Lu; Stephen A Kizito; Zhihai Qiu
Journal: Lipids Date: 2002-12 Impact factor: 1.880

2. Effects of antioestrogens on the DNA binding activity of oestrogen receptors in vitro.

Authors: N D Arbuckle; S Dauvois; M G Parker
Journal: Nucleic Acids Res Date: 1992-08-11 Impact factor: 16.971

3. Antiestrogen ICI 164,384 reduces cellular estrogen receptor content by increasing its turnover.

Authors: S Dauvois; P S Danielian; R White; M G Parker
Journal: Proc Natl Acad Sci U S A Date: 1992-05-01 Impact factor: 11.205

4. Inhibition of estrogen receptor-DNA binding by the "pure" antiestrogen ICI 164,384 appears to be mediated by impaired receptor dimerization.

Authors: S E Fawell; R White; S Hoare; M Sydenham; M Page; M G Parker
Journal: Proc Natl Acad Sci U S A Date: 1990-09 Impact factor: 11.205

5. Antagonists for Constitutively Active Mutant Estrogen Receptors: Insights into the Roles of Antiestrogen-Core and Side-Chain.

Authors: Abhishek Sharma; Weiyi Toy; Valeria Sanabria Guillen; Naina Sharma; Jian Min; Kathryn E Carlson; Christopher G Mayne; Shengjia Lin; Michael Sabio; Geoffrey Greene; Benita S Katzenellenbogen; Sarat Chandarlapaty; John A Katzenellenbogen
Journal: ACS Chem Biol Date: 2018-11-26 Impact factor: 5.100

10. Synthesis of novel estrogen receptor antagonists using metal-catalyzed coupling reactions and characterization of their biological activity.

Authors: Xiang-Rong Jiang; Pan Wang; Carolyn L Smith; Bao Ting Zhu
Journal: J Med Chem Date: 2013-03-26 Impact factor: 7.446

Novel steroidal pure antiestrogens.

1. New chemical syntheses of cholest-4,6-dien-3-one.

2. Effects of antioestrogens on the DNA binding activity of oestrogen receptors in vitro.

3. Antiestrogen ICI 164,384 reduces cellular estrogen receptor content by increasing its turnover.

4. Inhibition of estrogen receptor-DNA binding by the "pure" antiestrogen ICI 164,384 appears to be mediated by impaired receptor dimerization.

5. Antagonists for Constitutively Active Mutant Estrogen Receptors: Insights into the Roles of Antiestrogen-Core and Side-Chain.

Review 6. Transcription factors as drug targets: opportunities for therapeutic selectivity.

7. Synthesis and biological activity of 3-N-substituted estrogen derivatives as breast cancer agents.

8. Convergent synthesis of a deuterium-labeled serine dipeptide lipid for analysis of biological samples.

9. Specific mutations in the estrogen receptor change the properties of antiestrogens to full agonists.

10. Synthesis of novel estrogen receptor antagonists using metal-catalyzed coupling reactions and characterization of their biological activity.