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

被引：54

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

页码：306 / 316

页数：11

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