European Journal of Medicinal Chemistry p. 191 - 200 (2013)
Update date:2022-08-03
Topics:
Xu, Fuming
Zhang, Lei
Jia, Yuping
Wang, Xuejian
Li, Xiaoguang
Wen, Qingli
Zhang, Yingjie
Xu, Wenfang
A novel series of 4-amino-2-(thio)phenol derivatives were well synthesized. The preliminary biological test revealed that several compounds displayed high specific protein kinase and angiogenesis inhibitory activities compared with previous work mainly because of the substitution of sulfonamide structure for amide fragment. Among which, compound 5i was identified to inhibit protein kinase B/AKT (IC50 = 1.26 μM) and ABL tyrosine kinase (IC 50 = 1.50 μM) effectively. Meanwhile, compound 5i demonstrated competitive in vitro antiangiogenic activities to Pazopanib in both human umbilical vein endothelial cell (HUVEC) tube formation assay and the rat thoracic aorta rings test.
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