北京大学医学部机构知识库
Advanced  
IR@PKUHSC  > 北京大学药学院  > 期刊论文
学科主题: 药学
题名:
Novel sulfonanilide analogs decrease aromatase activity in breast cancer cells: Synthesis, biological evaluation, and ligand-based pharmacophore identification
作者: Su, Bin1; Tian, Ran2; Darby, Michael V.1; Brueggemeier, Robert W.1
刊名: JOURNAL OF MEDICINAL CHEMISTRY
发表日期: 2008-03-13
DOI: 10.1021/jm701107h
卷: 51, 期:5, 页:1126-1135
收录类别: SCI ; IC
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal
研究领域[WOS]: Pharmacology & Pharmacy
关键词[WOS]: SELECTIVE CYCLOOXYGENASE-2 INHIBITOR ; POSTMENOPAUSAL WOMEN ; EXPRESSION ; TAMOXIFEN ; NIMESULIDE ; THERAPY ; HYPERSENSITIVITY ; CHEMOPREVENTION ; APOPTOSIS ; RATS
英文摘要:

Aromatase converts androgens to estrogens and is a particularly attractive target in the treatment of estrogen receptor positive breast cancer. Previously, the COX-2 selective inhibitor nimesulide and analogs decreased aromatase expression and enzyme activity independent of COX-2 inhibition. In this manuscript, a combinatorial approach was used to generate diversely substituted novel sulfonanilides by parallel synthesis. Their pharmacological evaluation as agents for suppression of aromatase activity in SK-BR-3 breast cancer cells was extensively explored. A ligand-based pharmacophore model was elaborated for selective aromatase modulation (SAM) using the Catalyst HipHop algorithms. The best qualitative model consisted of four features: one aromatic ring, two hydrogen bond acceptors, and one hydrophobic function. Several lead compounds have also been tested in aromatase transfected MCF-7 cells, and they significantly suppressed cellular aromatase activity. The results suggest that both genomic and nongenomic mechanisms of these compounds are involved within the aromatase suppression effect.

语种: 英语
WOS记录号: WOS:000253784900005
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/49908
Appears in Collections:北京大学药学院_期刊论文

Files in This Item:

There are no files associated with this item.


作者单位: 1.Ohio State Univ, Coll Pharm, Div Med Chem & Pharmacognosy, Columbus, OH 43210 USA
2.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China

Recommended Citation:
Su, Bin,Tian, Ran,Darby, Michael V.,et al. Novel sulfonanilide analogs decrease aromatase activity in breast cancer cells: Synthesis, biological evaluation, and ligand-based pharmacophore identification[J]. JOURNAL OF MEDICINAL CHEMISTRY,2008,51(5):1126-1135.
Service
Recommend this item
Sava as my favorate item
Show this item's statistics
Export Endnote File
Google Scholar
Similar articles in Google Scholar
[Su, Bin]'s Articles
[Tian, Ran]'s Articles
[Darby, Michael V.]'s Articles
CSDL cross search
Similar articles in CSDL Cross Search
[Su, Bin]‘s Articles
[Tian, Ran]‘s Articles
[Darby, Michael V.]‘s Articles
Related Copyright Policies
Null
Social Bookmarking
Add to CiteULike Add to Connotea Add to Del.icio.us Add to Digg Add to Reddit

Items in IR are protected by copyright, with all rights reserved, unless otherwise indicated.

 

 

Valid XHTML 1.0!
Copyright © 2007-2017  北京大学医学部 - Feedback
Powered by CSpace