Discovery of 4-amino-2-(thio)phenol derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: Synthesis and biological evaluation. Part II

被引：12
|
作者：
Xu, Fuming [1 ]
Zhang, Lei [1 ]
Jia, Yuping [2 ]
Wang, Xuejian [1 ]
Li, Xiaoguang [1 ]
Wen, Qingli [3 ]
Zhang, Yingjie [1 ]
Xu, Wenfang [1 ]
机构：
[1] Shandong Univ, Sch Pharm, Dept Med Chem, Jinan 250012, Shandong, Peoples R China
[2] Shandong Inst Pharmaceut Ind, Jinan 250101, Shandong, Peoples R China
[3] Weifang Med Univ, Affiliated Hosp, Weifang 261031, Shandong, Peoples R China
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 69卷
关键词：
AKT; ABL; Protein kinase; HUVECs; Rat thoracic aorta rings; TUMOR-GROWTH; IN-VITRO; SULFONAMIDE; ANALOGS; DESIGN; AGENTS;
D O I：
10.1016/j.ejmech.2013.07.056
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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 mu M) and ABL tyrosine kinase (IC50 = 1.50 mu M) 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. (C) 2013 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：191 / 200
页数：10
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