β-Carbolines as specific inhibitors of cyclin-Dependent kinases

Y Song, J Wang, SF Teng, D Kesuma, Y Deng…

Index: Song, Yongcheng; Wang, Jian; Teng, Su Fern; Kesuma, Djohan; Deng, Yu; Duan, Jinao; Wang, Jerry H.; Qi, Robert Zhong; Sim, Mui Mui Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 7 p. 1129 - 1132

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Citation Number: 98

Abstract

Harmine (3), 7-fluoro-1-methyl β-carboline (35) and 1-(5-methyl-imidazol-4-yl) β-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 β-carbolines inhibited CDK2 and CDK5 to the same extent, selective inhibition against CDK2 was observed in 1-(2-chlorophenyl)-(12), 1-(2-fluorophenyl)-(15), ...