Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

Back

Design, Synthesis and Bioactivities of Phenylamino-Pyrimidine Derivatives as Novel Protein Tyrosine Kinase Inhibitors

Author(s): Xinfu Hong, Xianzhao Kuang, Guohua Ding, Yilin Liu, Jinlin Liu, Yanjin Zhao, Shuxin Li.

Abstract:

A series of novel phenylamino-pyrimidine derivatives were designed and synthesized as antitumor agent based on the lead compound of Imatinib by application of the principle of bioisosterism, hybridization and structural optimization. The bioactivities of the new target compounds were tested against human KU812 cells in vitro, some target compounds show promising activities and can be considered for further development.

Keywords: Protein tyrosine kinase, Phenylamino-pyrimidine, Synthesis, Bioactivity, Protein kinases, 2-phenylaminopyrimidine, bioisosterism, chronic myelogenous leukemia (CML), HNMR, DMSO-d6, tetramethylsilane (TMS), human KU812 cells, B ring, pharmacophores

Order Reprints Order Eprints Rights & PermissionsPrintExport

Article Details

VOLUME: 8
ISSUE: 7
Year: 2011
Page: [596 - 601]
Pages: 6
DOI: 10.2174/157018011796235202
Price: $58