Synthesis and biological evaluation of novel pazopanib derivatives as antitumor agents

被引：21

作者：

Qi, Haofei ^{[1
]}

Chen, Ligong ^{[1
]}

Liu, Bingni ^{[2
]}

Wang, Xinran ^{[1
]}

Long, Li ^{[3
]}

Liu, Dengke ^{[2
]}

机构：

[1] Tianjin Univ, Sch Chem Engn & Technol, Tianjin 300072, Peoples R China

[2] Tianjin Inst Pharmaceut Res, Tianjin Key Lab Mol Design & Drug Discovery, Tianjin 300193, Peoples R China

[3] Tianjin Polytech Univ, Sch Environm & Chem Engn, Tianjin 300387, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 04期

关键词：

Pazopanib derivatives; Synthesis; Tyrosine kinase; Inhibitory activity; TYROSINE KINASE INHIBITORS;

D O I：

10.1016/j.bmcl.2014.01.003

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel pazopanib derivatives, 7a-m, were designed and synthesized by modification of terminal benzene and indazole rings in pazopanib. The structures of all the synthesized compounds were confirmed by H-1 NMR and MS. Their inhibitory activity against VEGFR-2, PDGFR-alpha and c-kit tyrosine kinases were evaluated. All the compounds exhibited definite kinase inhibition, in which compound 7l was most potent with IC50 values of 12 nM against VEGFR-2. Furthermore, compounds 7c, 7d and 7m demonstrated comparable inhibitory activity against three tyrosine kinases to pazopanib, and compound 7f showed superior inhibitory effects than that of pazopanib. (C) 2014 Elsevier Ltd. All rights reserved.

引用

页码：1108 / 1110

页数：3

共 50 条

[1] Design, Synthesis and Biological Evaluation of Pazopanib Derivatives as Antitumor Agents
Jia, Yuping
Zhang, Jian
Feng, Jinhong
Xu, Fuming
Pan, Huili
Xu, Wenfang
[J]. CHEMICAL BIOLOGY & DRUG DESIGN, 2014, 83 (03) : 306 - 316
[2] Synthesis and Biological Evaluation of Novel Tetrahydroisoquinoline Derivatives as Antitumor Agents
Wang, Dao-Cai
Song, Hang
Yao, Shun
[J]. ASIAN JOURNAL OF CHEMISTRY, 2014, 26 (12) : 3493 - 3495
[3] Synthesis and Biological Evaluation of Novel Phenothiazine Derivatives as Potential Antitumor Agents
Venkatesan, K.
Satyanarayana, V. S. V.
Sivakumar, A.
[J]. POLYCYCLIC AROMATIC COMPOUNDS, 2023, 43 (01) : 850 - 859
[4] SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL PHOSPHONATES DERIVATIVES OF AS POTENTIAL ANTITUMOR AGENTS
Jin, Chuanfei
Liang, Yong-Ju
He, Hongwu
Fu, Liwu
[J]. PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS, 2011, 186 (10) : 2096 - 2103
[5] Design, synthesis and biological evaluation of valepotriate derivatives as novel antitumor agents
Zhang, Bo
Guo, Ruiying
Hu, Yongzhou
Dong, Xiaowu
Lin, Nengming
Dai, Xiaoyang
Wu, Honghai
Ma, Shenglin
Yang, Bo
[J]. RSC ADVANCES, 2017, 7 (51): : 31899 - 31906
[6] Synthesis and Biological Evaluation of Novel Acenaphthene Derivatives as Potential Antitumor Agents
Xie, Yong-Mei
Deng, Yi
Dai, Xiao-Yun
Liu, Jie
Ouyang, Liang
Wei, Yu-Quan
Zhao, Ying-Lan
[J]. MOLECULES, 2011, 16 (03) : 2519 - 2526
[7] Synthesis and biological evaluation of novel indoleamide derivatives as antioxidative and antitumor agents
Zhang, Zhen
Gu, Ying-Lin
Wang, Zheng-Yang
Wang, Huan-Nan
Zhao, Yan
Chu, Xue-Mei
Zhang, Chun-Yan
Yan, Mao-Cai
[J]. JOURNAL OF HETEROCYCLIC CHEMISTRY, 2020, 57 (03) : 1165 - 1172
[8] Synthesis and biological evaluation of novel acylhydrazone derivatives as potential antitumor agents
Congiu, Cenzo
Onnis, Valentina
[J]. BIOORGANIC & MEDICINAL CHEMISTRY, 2013, 21 (21) : 6592 - 6599
[9] Synthesis and Biological Evaluation of Novel Tricyclic Oximino Derivatives as Antitumor Agents
GUO Shu-chun
[J]. Chemical Research in Chinese Universities, 2008, (01) : 47 - 53
[10] Synthesis and biological evaluation of novel tricyclic oximino derivatives as antitumor agents
Guo Shu-chun
Zhao Yan-fang
Li Rong-dong
Xie Li-jun
Yang You-bin
Gong Ping
[J]. CHEMICAL RESEARCH IN CHINESE UNIVERSITIES, 2008, 24 (01) : 47 - 53

← 1 2 3 4 5 →