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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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 and Shuxin Li

Volume 8, Issue 7, 2011

Page: [596 - 601] Pages: 6

DOI: 10.2174/157018011796235202

Price: $65

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


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