Synthesis of Pyrazolo[3,4-d]pyrimidine Derivatives and Evaluation of their Src Kinase Inhibitory Activities

Authors

Anil Kumar, Birla Institute of Technology & ScienceFollow
Guofeng Ye, Shandong UniversityFollow
Xianfeng Gu, SUNY Stony Brook
Yuehao Wang, University of Rhode IslandFollow
Gongqin Sun, University of JinanFollow
Keykavous Parang, Chapman UniversityFollow

Document Type

Article

Publication Date

2013

Abstract

A series of pyrazolo[3,4-d]pyrimidine derivatives was synthesized and evaluated for the Src kinase inhibitory activities. Compound 6e and 10c exhibited inhibition of Src kinase with an IC50 value of 5.6 and 5.1 μM, respectively. Hydroxamate derivative 15a was found to be a metal-mediated inhibitor for human Csk with an IC50 value of 2.0 μM showing 56-fold selectivity over Src kinase inhibition.

Comments

This article was originally published in Chemistry & Biology Interface , in 2013.

Recommended Citation

Kumar, A., Ye, G., Gu, X., Wang, Y., Sun, G., Parang K. Synthesis of pyrazolo[3,4-d]pyrimidine derivatives and evaluation of their Src kinase inhibitory activities. Chemistry & Biology Interface (2013) 3, 264-269.

Copyright

Indian Society of Chemists and Biologists