Aurora kinase A inhibitors:: Identification, SAR exploration and molecular modeling of 6,7-dihydro-4H-pyrazolo-[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione scaffold

被引：28

作者：

Coumar, Mohane Selvaraj ^{[1
]}

Wu, Jian-Sung ^{[1
]}

Leou, Jiun-Shyang ^{[1
]}

Tan, Uan-Kang ^{[2
]}

Chang, Chung-Yu ^{[1
]}

Chang, Teng-Yuan ^{[1
]}

Lin, Wen-Hsing ^{[1
]}

Hsu, John T. -A. ^{[1
,3
]}

Chao, Yu-Sheng ^{[1
]}

Wu, Su-Ying ^{[1
]}

Hsieh, Hsing-Pang ^{[1
]}

机构：

[1] Natl Hlth Res Inst, Div Biotechnol & Pharmaceut Res, Zhunan Town 350, Miaoli County, Taiwan

[2] Technol & Sci Inst No Taiwan, Dept Chem & Mat Engn, Taipei 112, Taiwan

[3] Natl Tsing Hua Univ, Dept Chem Engn, Hsinchu 300, Taiwan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 05期

关键词：

aurora kinase inhibitors; cancer; molecular modeling;

D O I：

10.1016/j.bmcl.2008.01.068

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Tricyclic 6,7-dihydro-4H-pyrazolo[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione was identified as a novel scaffold for Aurora kinase A inhibition through virtual screening. SAR exploration coupled with molecular modeling of 8a reveals the minimum pharmacophore requirements for Aurora kinase A inhibition. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：1623 / 1627

页数：5

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