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

被引：51
|
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：
国家高技术研究发展计划(863计划); 中国国家自然科学基金;
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
下载
收藏
页码：306 / 316
页数：11
相关论文
共 50 条
  • [31] Synthesis, Structure and Biological Evaluation of Thiourea Derivatives as Antitumor Agents
    Quo Feng-Jiao
    Sun Juan
    Zhou Wei
    Zhu Hai-Liang
    CHINESE JOURNAL OF STRUCTURAL CHEMISTRY, 2014, 33 (01) : 79 - 84
  • [32] Synthesis and Biological Evaluation of Novel Tetrahydroisoquinoline Derivatives as Antitumor Agents
    Wang, Dao-Cai
    Song, Hang
    Yao, Shun
    ASIAN JOURNAL OF CHEMISTRY, 2014, 26 (12) : 3493 - 3495
  • [33] Synthesis and biological evaluation of podophyllotoxin derivatives as selective antitumor agents
    Wu, Gao-Rong
    Xu, Bing
    Yang, Yu-Qin
    Zhang, Xin-Yu
    Fang, Kang
    Ma, Tao
    Wang, Hui
    Xue, Nan-Nan
    Chen, Meng
    Guo, Wen-Bo
    Jia, Xiao-Hui
    Wang, Peng-Long
    Lei, Hai-Min
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2018, 155 : 183 - 196
  • [34] Synthesis,Structure and Biological Evaluation of Thiourea Derivatives as Antitumor Agents
    郭凤娇
    孙娟
    周伟
    朱海亮
    Chinese Journal of Structural Chemistry, 2014, (01) : 79 - 84
  • [35] Synthesis,Structure and Biological Evaluation of Thiourea Derivatives as Antitumor Agents
    郭凤娇
    孙娟
    周伟
    朱海亮
    结构化学, 2014, 33 (01) : 79 - 84
  • [36] Design, synthesis, and biological antitumor evaluation of tetrahydroisoquinoline derivatives
    Pang, Can
    Zhao, Jianbo
    Zhang, Shuai
    Chen, Jiayu
    Zeng, Xiu
    Li, Hao
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2024, 109
  • [37] Design, Synthesis and Biological Evaluation of C(6)-Modified Celastrol Derivatives as Potential Antitumor Agents
    Tang, Kaiyong
    Huang, Qingqing
    Zeng, Jafeng
    Wu, Guangming
    Huang, Jinwen
    Pan, Junfang
    Lu, Wei
    MOLECULES, 2014, 19 (07) : 10177 - 10188
  • [38] Design, Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives Bearing Semicarbazone Moiety as Antitumor Agents
    Ma Junjie
    Hu Gang
    Xie Lijun
    Chen Lei
    Xu Boxuan
    Gong Ping
    CHEMICAL RESEARCH IN CHINESE UNIVERSITIES, 2015, 31 (06) : 958 - 963
  • [39] Design, synthesis and biological evaluation of novel carbohydrate-based sulfonamide derivatives as antitumor agents
    Hao, Shuang
    Cheng, Xue
    Wang, Xin
    An, Ran
    Xu, Hang
    Guo, Mengbi
    Li, Chuanchao
    Wang, Yitong
    Hou, Zhuang
    Guo, Chun
    BIOORGANIC CHEMISTRY, 2020, 104
  • [40] Design, synthesis and biological evaluation of novel furoxan-based coumarin derivatives as antitumor agents
    Zhuo Zhang
    Zhi-Wei Bai
    Yong Ling
    Li-Qin He
    Peng Huang
    Hong-Xia Gu
    Rong-Feng Hu
    Medicinal Chemistry Research, 2018, 27 : 1198 - 1205
12345