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KMID : 0043320140370070873
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Archives of Pharmacal Research
2014 Volume.37 No. 7 p.873 ~ p.881
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Novel 2,4-dianilino-5-fluoropyrimidine derivatives possessing ALK inhibitory activities
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Yun Jeong-In
Yang Eun-Hye
Latif Muhammad
Lee Hyeon-Ji
Lee Kwang-Ho
Yun Chang-Soo
Park Chi-Hoon
Lee Chong-Ock
Chae Chong-Hak
Cho Sung-Yun
Jung Hee-Jung
Kim Pil-Ho
Choi Sang-Un
Kim Hyoung-Rae
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Abstract
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A new series of 2,4-dianilino-5-fluoropyrimidine derivatives were designed and synthesized and their anaplastic lymphoma kinase (ALK) inhibitory activities were evaluated by biochemical and cell-based assays in order to discover a new ALK inhibitor. Most compounds synthesized showed good inhibitory activities against ALK and good cytotoxic activities in H3122 cell line. The best compound 6f showed good activity against wild-type ALK along with crizotinib-resistant mutant ALK, and it showed 6 times better activity in cell-based assay than crizotinib. Some SAR studies were performed by the comparisons of the activities between 6 and the designed-synthesized compounds.
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KEYWORD
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Anaplastic lymphoma kinase, ALK inhibitor, Pyrimidine derivatives, Kinase inhibitor, Anti-cancer agent, 2, 4-Dianilino-5-Fluoropyrimidine
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