Selenophenes: Introducing a New Element into the Core of Non-Steroidal Estrogen Receptor Ligands

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作者信息关键词期刊信息基础信息归属信息摘要

成果类型：

期刊论文

作者：

Zhang, Silong;Wang, Zhiyong;Hu, Zhiye;Li, Changhao;Tang, Chu;...

通讯作者：

Zhou, Hai-Bing;Huang, Jian

作者机构：

[Zhang, Silong; Zhou, Hai-Bing; Tang, Chu; Wang, Zhiyong; Dong, Chune; Luo, Junjie; Hu, Zhiye] Wuhan Univ, State Key Lab Virol, Key Lab Combinatorial Biosynth & Drug Discovery, Sch Pharmaceut Sci,Minist Educ, 185 East Lake Rd, Wuhan 430071, Peoples R China.

[Li, Changhao; Huang, Jian] Wuhan Univ, Coll Life Sci, 299 Bayi Rd, Wuhan 430072, Peoples R China.

[Carlson, Kathryn E.; Katzenellenbogen, John A.] Univ Illinois, Dept Chem, 600 South Mathews Ave, Urbana, IL 61801 USA.

[Zhou, Hai-Bing] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.

通讯机构：

[Zhou, Hai-Bing; Huang, Jian] W

[Zhou, Hai-Bing] U

Wuhan Univ, State Key Lab Virol, Key Lab Combinatorial Biosynth & Drug Discovery, Sch Pharmaceut Sci,Minist Educ, 185 East Lake Rd, Wuhan 430071, Peoples R China.

Wuhan Univ, Coll Life Sci, 299 Bayi Rd, Wuhan 430072, Peoples R China.

Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China.

语种：

英文

关键词：

breast cancer;estrogen receptor;structural diversity;relative binding affinity;selenophenes

期刊：

ChemMedChem

ISSN：

1860-7179

年：

2017

卷：

期：

页码：

235-249

DOI：

10.1002/cmdc.201600593

基金类别：

NSFCNational Natural Science Foundation of China (NSFC) [81373255, 31371331, 81573279]; Key Scientific Research Project of Ministry of Education of ChinaMinistry of Education, China [313040]; Hubei Province's Outstanding Medical Academic Leader Program; Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals; US National Institutes of HealthUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) - USA [PHS 5R01 DK015556]; NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASESUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) - USANIH National Institute of Diabetes & Digestive & Kidney Diseases (NIDDK) [R01DK015556, R01DK015556, R01DK015556, R01DK015556, R01DK015556] Funding Source: NIH RePORTER

机构署名：

本校为通讯机构

院系归属：

药学与生物科学学院

摘要：

The importance of the heterocyclic core elements with peripheral phenolic and alkyl substituents as a dominant structural motif of ligands for the estrogen receptor (ER) has been well recognized. In this study we expanded the structural diversity of core elements by preparing selenium-containing heterocycles and exploring the activities of these selenophenes on the two ERs, ERα and ERβ. Careful structure–activity relationship (SAR) analysis of their ER binding affinities showed that most selenophenes are ERβ-selective, with the position of ...

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Selenophenes: Introducing a New Element into the Core of Non-Steroidal Estrogen Receptor Ligands

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