Synthesis and evaluation of new thiourea derivatives as antitumor and antiangiogenic agents

NWIPB OpenIR

	Synthesis and evaluation of new thiourea derivatives as antitumor and antiangiogenic agents
	Bai, Wenjing; Ji, Jianxin; Huang, Qiang; Wei, Wei
	2020
发表期刊	TETRAHEDRON LETTERS
卷号	61 期号:40
摘要	A series of novel thiourea derivatives were synthesized and evaluated by biological activities. Among them, compound 10e containing 3,5-bis(trifluoromethyl)phenyl moiety (R-1) at the terminal thiourea and phenylamino (R-2) at the terminal acyl position showed the best cytotoxic activities against seven cancer cell lines (NCI-H460, Colo-205, HCT116, MDA-MB-231, MCF-7, HepG2, PLC/PRF/5) and HUVECs. Moreover, compound 10e moderately inhibited various RTKs such as VEGFR2, VEGFR3, and PDGFR beta. Notably, 10e exhibited much better inhibitory effect of tumor formation and antiangiogenic activities than Sorafenib and Regorafenib at the same concentration. Further docking studies suggested that 10e could serve as potential candidate for cancer therapy. (C) 2020 Elsevier Ltd. All rights reserved.
关键词	Thiourea derivatives Antitumor Antiangiogenesis RTK inhibitors
文献类型	期刊论文
条目标识符	http://210.75.249.4/handle/363003/60237
专题	中国科学院西北高原生物研究所
推荐引用方式 GB/T 7714	Bai, Wenjing,Ji, Jianxin,Huang, Qiang,et al. Synthesis and evaluation of new thiourea derivatives as antitumor and antiangiogenic agents[J]. TETRAHEDRON LETTERS,2020,61(40).
APA	Bai, Wenjing,Ji, Jianxin,Huang, Qiang,&Wei, Wei.(2020).Synthesis and evaluation of new thiourea derivatives as antitumor and antiangiogenic agents.TETRAHEDRON LETTERS,61(40).
MLA	Bai, Wenjing,et al."Synthesis and evaluation of new thiourea derivatives as antitumor and antiangiogenic agents".TETRAHEDRON LETTERS 61.40(2020).