Bioorganic & Medicinal Chemistry Letters 2008-04-01

Synthesis and biological evaluation of 3,5-diaminoindazoles as cyclin-dependent kinase inhibitors.

Jinho Lee, Hwangeun Choi, Kyoung-Hee Kim, Shinwu Jeong, Jong-Wook Park, Chul-Su Baek, Sei-Hee Lee

Index: Bioorg. Med. Chem. Lett. 18(7) , 2292-5, (2008)

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Abstract

A novel series of 3,5-diaminoindazoles were prepared and found to be CDK inhibitors. Potent inhibitors against CDK1 and CDK2 were obtained by introduction of 1lambda(6)-isothiazolidine-1,1-dioxide at 5-position of indazole. Anti-proliferative activities of compounds were evaluated using EJ, HCT116, SW620, and A549 cancer cell lines.