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Published on: January 27, 2026
Novel 2,4-dianilino-5-fluoropyrimidine derivatives possessing ALK inhibitory activities
Jeong In Yun1, Eun Hye Yang, Muhammad Latif
1Korea Research Institute of Chemical Technology, 141 Gajeongro, Yuseong, Daejeon, 305-600, Korea.
Abstract:
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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