Synthesis and biological evaluations of pyrazolo [3, 4-d] pyrimidines as cyclin-dependent kinase 2 inhibitors

…, YR Lee, BS Yang, KJ Shin, DJ Kim, BY Chung…

Index: Kim, Dong Chan; Lee, Yeo Ran; Yang, Beom-Seok; Shin, Kye Jung; Kim, Dong Jin; Chung, Bong Young; Yoo, Kyung Ho European Journal of Medicinal Chemistry, 2003 , vol. 38, # 5 p. 525 - 532

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Citation Number: 83

Abstract

A series of 1, 4, 6-trisubstituted pyrazolo [3, 4-d] pyrimidines 15–19, 30–38 capable of selectively inhibiting CDK2 activity were synthesized by derivatization at C-4, C-6 and N-1 with various amines and lower alkyl groups. For above synthetic compounds, biological evaluation was carried out and structure–activity relationship was examined. In our series, 4- anilino compounds exhibited better CDK2 inhibitory activity and antitumor activity ...