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Novel sulfonanilide analogs decrease aromatase activity in breast cancer cells: Synthesis, biological evaluation, and ligand-based pharmacophore identification
Su, Bin1; Tian, Ran2; Darby, Michael V.1; Brueggemeier, Robert W.1
刊名JOURNAL OF MEDICINAL CHEMISTRY
2008-03-13
DOI10.1021/jm701107h
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
Cited Times:19[WOS]   [WOS Record]     [Related Records in WOS]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/49908
Collection北京大学药学院
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
GB/T 7714
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.
APA Su, Bin,Tian, Ran,Darby, Michael V.,&Brueggemeier, Robert W..(2008).Novel sulfonanilide analogs decrease aromatase activity in breast cancer cells: Synthesis, biological evaluation, and ligand-based pharmacophore identification.JOURNAL OF MEDICINAL CHEMISTRY,51(5),1126-1135.
MLA Su, Bin,et al."Novel sulfonanilide analogs decrease aromatase activity in breast cancer cells: Synthesis, biological evaluation, and ligand-based pharmacophore identification".JOURNAL OF MEDICINAL CHEMISTRY 51.5(2008):1126-1135.
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