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

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

Volume: 8 Issue: 7

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

Affiliation:

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

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.

Cite this article as:

Hong Xinfu, Kuang Xianzhao, Ding Guohua, Liu Yilin, Liu Jinlin, Zhao Yanjin and Li Shuxin, Design, Synthesis and Bioactivities of Phenylamino-Pyrimidine Derivatives as Novel Protein Tyrosine Kinase Inhibitors, Letters in Drug Design & Discovery 2011; 8 (7) . https://dx.doi.org/10.2174/157018011796235202