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【论文发表】Discovery of 6-arylurea-2-arylbenzoxazole and 6-arylurea-2-arylbenzimidazole derivatives as angiogenesis inhibitors: design, synthesis and in vitro biological evaluation

2019年06月03日 16:09  点击:[]

Discovery of 6-arylurea-2-arylbenzoxazole and 6-arylurea-2-arylbenzimidazole derivatives as angiogenesis inhibitors: design, synthesis and in vitro biological evaluation.

By: Jin, Yi; Zi, Mengli; Liu, Feifei; Wu, Di; Li, Ke; Zhang, Da; Zhu, Changcheng; Zhang, ZhiYun; Li, Linghua; Zhang, Conghai; Xie, Mingjin; Lin, Jun; Zhang, Jihong.

Chem Med Chem (International ed. in English)

DOI: 10.1002/cmdc.201900216

Published: 26 May 2019

Document Type:Journal Article

Abstract

Herein, we embarked on a structural optimization campaign aiming at the discovery of novel anti-angiogenesis agents with previously reported imidazole kinase inhibitors as a lead compound. A library of 29 compounds has been synthesized. Several title compounds exhibited selective inhibitory activities against VEGFR-2 kinase than EGFR kinases, which also displayed selective anti-proliferation potency against three cancer cells. The newly synthesized compounds were evaluated for anti-angiogenesis capability by CAM assay. Among them, compound 5n showed the most potent anti-angiogenesis ability, the efficient cytotoxic activities (in vitro against HUVEC, H1975, A549 and Hela cell lines with IC50 values of 8.46, 1.40, 7.61, and 0.28 M, respectively), and acceptable VEGFR-2 kinase inhibition (IC50 = 0.25 M). The molecular docking analysis revealed d 5n is a Type II inhibitor of VEGFR-2 kinase. In general, these results indicated these 6-arylurea-2-arylbenzoxazole/

benzimidazole derivatives are promising inhibitors of VEGFR-2 kinase for the potential treatment of anti-angiogenesis.

Keywords

Antiangiogenesis; VEGFR-2 kinase inhibitors; benzimidazole; benzoxazole

Author Information

YunNan University, Key Laboratory of Medicinal Chemistry for Natural Resource, NO.5 north of Cuihu Road, 650091, Kunming, CHINA. CHINA.

全文链接: https://sci-hub.tw/10.1002/cmdc.201900216

   

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