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Letters in Drug Design & Discovery

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

DOI: 10.2174/157018011796235202

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

Page: [596 - 601] Pages: 6

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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