Lead optimization to improve the antiviral potency of 2-aminobenzamide derivatives targeting HIV-1 Vif-A3G axis

	Lead optimization to improve the antiviral potency of 2-aminobenzamide derivatives targeting HIV-1 Vif-A3G axis
	Zhong, XX; Luo, RH; Yan, GY; Ran, K; Shan, HF; Yang, J; Liu, YY; Yu, S; Pu, CL; Zheng, YT; Li, R
	2021
发表期刊	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN	0223-5234
卷号	224
摘要	The viral infectivity factor (Vif)-apolipoprotein B mRNA-editing enzyme, catalytic polypeptide-like 3G (APOBEC3G) axis has been recognized as a valid target for developing novel small-molecule therapies for acquired immune deficiency syndrome (AIDS) or for enhancing innate immunity against viruses. Our previous work reported the novel Vif antagonist 2-amino-N-(2-methoxyphenyl)-64(4-nitrophenyl)sulfonyllbenzamide (2) with strong antiviral activity. In this work, through optimizations of ring C of 2, we discovered the more potent compound 6m with an EC50 of 0.07 mu M in non-permissive H9 cells, reflecting an approximately 5-fold enhancement of antiviral activity compared to that of 2. Western blotting indicated that 6m more strongly suppressed the defensive protein Vif than 2 at the same concentration. Furthermore, 6m suppressed the replication of various clinical drug-resistant HIV strains (FI, NRTI, NNRTI, IN and PI) with relatively high efficacy. These results suggested that compound 6m is a more potent candidate for treating AIDS. (C) 2021 Elsevier Masson SAS. All rights reserved.
收录类别	sci
语种	英语
文献类型	期刊论文
条目标识符	http://ir.kiz.ac.cn/handle/152453/13824
专题	科研部门_分子免疫药理学（郑永唐）
推荐引用方式 GB/T 7714	Zhong, XX,Luo, RH,Yan, GY,et al. Lead optimization to improve the antiviral potency of 2-aminobenzamide derivatives targeting HIV-1 Vif-A3G axis[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2021,224.
APA	Zhong, XX.,Luo, RH.,Yan, GY.,Ran, K.,Shan, HF.,...&Li, R.(2021).Lead optimization to improve the antiviral potency of 2-aminobenzamide derivatives targeting HIV-1 Vif-A3G axis.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,224.
MLA	Zhong, XX,et al."Lead optimization to improve the antiviral potency of 2-aminobenzamide derivatives targeting HIV-1 Vif-A3G axis".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 224(2021).

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