Incorporation of a rigid 1,3-diketone-containing fragment led to significantly improved AXL inhibitory activity: design, synthesis, and SAR of the anilinopyrimidine AXL inhibitors.

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Title: Incorporation of a rigid 1,3-diketone-containing fragment led to significantly improved AXL inhibitory activity: design, synthesis, and SAR of the anilinopyrimidine AXL inhibitors.
Authors: Hu W; School of Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing, 210023, Jiangsu, People's Republic of China., Peng X; Division of Antitumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai, 201203, Jiangsu, People's Republic of China., Ji Y; Division of Antitumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai, 201203, Jiangsu, People's Republic of China., Duan W; Small-Molecule Drug Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai, 201203, People's Republic of China.; School of Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing, 210023, Jiangsu, People's Republic of China.; University of Chinese Academy of Sciences, No. 19A Yuquan Road, Beijing, 1000449, People's Republic of China., Ai J; Division of Antitumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai, 201203, Jiangsu, People's Republic of China. jai@simm.ac.cn.; University of Chinese Academy of Sciences, No. 19A Yuquan Road, Beijing, 1000449, People's Republic of China. jai@simm.ac.cn., Zhan Z; Small-Molecule Drug Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai, 201203, People's Republic of China. zszhan@simm.ac.cn.; School of Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing, 210023, Jiangsu, People's Republic of China. zszhan@simm.ac.cn.; University of Chinese Academy of Sciences, No. 19A Yuquan Road, Beijing, 1000449, People's Republic of China. zszhan@simm.ac.cn.
Source: Molecular diversity [Mol Divers] 2025 Oct; Vol. 29 (5), pp. 4627-4643. Date of Electronic Publication: 2024 Dec 28.
Publication Type: Journal Article
Journal Info: Publisher: ESCOM Science Publishers Country of Publication: Netherlands NLM ID: 9516534 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1573-501X (Electronic) Linking ISSN: 13811991 NLM ISO Abbreviation: Mol Divers Subsets: MEDLINE
Database: MEDLINE Ultimate
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ISSN:1573-501X
DOI:10.1007/s11030-024-11071-9