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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

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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.
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