Design, Synthesis and Biological Evaluation of Pazopanib Derivatives as Antitumor Agents

被引：53
|
作者：
Jia, Yuping [1 ]
Zhang, Jian [2 ]
Feng, Jinhong [3 ]
Xu, Fuming [2 ]
Pan, Huili [2 ]
Xu, Wenfang [2 ]
机构：
[1] Shandong Inst Pharmaceut Ind, Jinan 250101, Shandong, Peoples R China
[2] Shandong Univ, Dept Med Chem, Sch Pharmaceut Sci, Jinan 250012, Shandong, Peoples R China
[3] Shandong Acad Sci, Shandong Anal & Test Ctr, Jinan 250012, Shandong, Peoples R China
来源：
CHEMICAL BIOLOGY & DRUG DESIGN | 2014年 / 83卷 / 03期
基金：
中国国家自然科学基金; 国家高技术研究发展计划(863计划);
关键词：
anti-angiogenesis; antitumor agent; pazopanib derivatives; synthesis; ENDOTHELIAL GROWTH-FACTOR; ANGIOGENESIS; INHIBITORS; MECHANISMS; THERAPY; KINASES; TARGET; CELLS;
D O I：
10.1111/cbdd.12243
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
A novel series of pazopanib derivatives were designed, synthesized, and evaluated for their inhibitory activity against a series of kinases including VEGFR-2, EGFR, AKT1, ALK1, and ABL1. The anti-angiogenic activities ex vivo of some compounds were also investigated. Compounds P2d and P2e demonstrated outstanding inhibitory activity against VEGFR-2 and ABL1 and higher anti-angiogenic activity compared with Pazopanib, the reference standard. These two compounds (P2d and P2e) could be used as novel lead compounds for further development of anticancer agents.
引用
收藏
页码：306 / 316
页数：11
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