Bioorganic and Medicinal Chemistry p. 4735 - 4744 (2018)
Update date:2022-07-29
Topics: Synthesis Design Structure Structure-Activity Relationship Experimental Diaryl-ureas Receptor tyrosine kinase Isoxazol[3,4-b]pyridine-3-amino-structure Multi-target inhibitors
Shi, Zhi-Hao
Liu, Feng-Tao
Tian, Hao-Zhong
Zhang, Yan-Min
Li, Nian-Guang
Lu, Tao
Inspired by that the multi-target inhibitors against receptor tyrosine kinases (RTKs) have significantly improved the effect of clinical treatment for cancer, and based on the chemical structure of Linifanib (ABT-869, Abbott), two series of diaryl-ureas with novel isoxazol[3,4-b]pyridine-3-amino-structure were designed and synthesized as multi-target inhibitors against RTKs. The preliminary biological evaluation showed that several compounds exhibited comparable potency with Linifanib. Compound S21 was identified as the most potent inhibitor against Fms-like tyrosine kinase 3 (FLT-3), kinase insert domain containing receptor (KDR) and platelet-derived growth factor receptor β (PDGFR-β) with its IC50 values were 4 nM, 3 nM and 8 nM respectively, it also showed potent inhibitory activities against several cancer cells.
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