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β-Carbolines as specific inhibitors of cyclin-dependent kinases

被引：143
作者：
Song, YC
Wang, J
Teng, SF
Kesuma, D
Deng, Y
Duan, JN
Wang, JH
Qi, RZ
Sim, MM
机构：
[1] Inst Mol & Cell Biol, Med & Combinatorial Chem Grp, Singapore 117609, Singapore
[2] Inst Mol & Cell Biol, Funct Proteom Grp, Singapore 117609, Singapore
[3] Hong Kong Univ Sci & Technol, Dept Biochem, Kowloon, Hong Kong, Peoples R China
[4] Hong Kong Univ Sci & Technol, Biotechnol Res Inst, Kowloon, Hong Kong, Peoples R China
[5] China Pharmaceut Univ, Nanjing, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 07期
关键词：
D O I：
10.1016/S0960-894X(02)00094-X
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Harmine (3), 7-fluoro-1-methyl beta-carboline (35) and 1-(5-methyl-imidazol-4-yl) beta-carboline (41) were potent and specific inhibitors of cyclin-dependent kinases. The degree of aromaticity of the tricyclic ring and the positioning of substituents are important for inhibitory activity. While most beta-carbolines inhibited CDK2 and CDK5 to the same extent. selective inhibition against CDK2 was observed in 1-(2-chlorophenyl)- (12), 1-(2-fluorophenyl)- (15), and 1-(2-chloro-5-nitrophenyl)- (28) beta-carbolines. (C) 2002 Elsevier Science Ltd. All rights reserved.
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收藏
页码：1129 / 1132
页数：4
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