您當前的位置: 首頁 >> 科研成果 >> 正文

【論文發表】Discovery of arylamide-5-anilinoquinazoline-8-nitro derivatives as VEGFR-2 kinase inhibitors: synthesis, in vitro biological evaluation and molecular docking

2019年10月21日 16:19  點擊:[]

Discovery of arylamide-5-anilinoquinazoline-8-nitro derivatives as VEGFR-2 kinase inhibitors: synthesis, in vitro biological evaluation and molecular docking

By: Yongqiang Zhao, Feifei Liu, Guojing He, Ke Li, Changcheng Zhu, Wei Yu, Conghai Zhang, Mingjin Xie, Jun Lin, Jihong Zhang, Yi Jin

Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming, 650091, P. R. China

Laboratory of Molecular Genetics of Aging and Tumor, Medical School, Kunming University of Science and Technology, Kunming, 650500, P. R. China

Biomedical Department, Yunnan Cancer Hospital, the Third Affiliated Hospital of Kunming Medical University, Kunming, 650118, P. R. China

Institute of Drug Research and Development, Kunming Pharmaceutical Corporation, Kunming, 650100, P. R. China

Pharmaceutical Department, Kunming General Hospital of Chengdu Military Command, Kunming, 650118, P. R. ChinaBioorganic & Medicinal Chemistry Letters, Available Online

Bioorganic & Medicinal Chemistry Letters, Available Online

doi.org/10.1016/j.bmcl.2019.126711

Publication Date (Web): October 19, 2019

Document Type: Article

Abstract

Herein, we embarked on a structural optimization campaign aiming at the discovery of novel anticancer agents with our previously reported XL-6f as a lead compound. A library of 23 compounds has been synthesized based on the highly conserved active site of VEGFR-2. Several title compounds exhibited selective inhibitory activities against VEGFR-2, which also displayed selective anti-proliferation potency against HepG2 cell. All synthesized compounds were evaluated for anti-angiogenesis capability. Compound 7o showed the most potent anti-angiogenesis ability, the efficient cytotoxic activities (in vitro against HUVEC and HepG2 cell lines with IC50 values of 0.58 and 0.23 μM, respectively). The molecular docking analysis revealed 7o is a Type-II inhibitor of VEGFR-2 kinase. In general, these results indicated these arylamide-5-anilinoquinazoline-8-nitro derivatives are promising inhibitors of VEGFR-2 for the potential treatment of anti-angiogenesis.

全文鏈接:

https://www.sciencedirect.com/science/article/pii/S0960894X19306699

下一條:【論文發表】Tandem reaction of heterocyclic ketene aminals with diazoesters: Synthesis of pyrimidopyrrolidone derivatives

關閉

聯系我們
  • 電話:0871-65031119
  • 地址:昆明市翠湖北路2號
色三级床上片电影完整版- 视频 - 在线观看 - 影视资讯 - 爱赏网