NDLI: Design, synthesis and biological evaluation of indolizine derivatives as HIV-1 VIF

Content Provider	Springer Nature Link
Author	Huang, Wenlin Zuo, Tao Jin, Hongwei Liu, Zhenming Yang, Zhenjun Yu, Xianghui Zhang, Liangren Zhang, Lihe
Copyright Year	2013
Abstract	The HIV-1 viral infectivity factor (VIF) protein is essential for viral replication. VIF recruits cellular ElonginB/C-Cullin5 E3 ubiquitin ligase to target the host antiviral protein APOBEC3G (A3G) for proteasomal degradation. Thus, the A3G-Vif–E3 complex represents an attractive target for the development of novel anti-HIV drugs. In this study, we describe the design and synthesis of indolizine derivatives as VIF inhibitors targeting the VIF–ElonginC interaction. Many of the synthesized compounds exhibited obvious inhibition activities of VIF-mediated A3G degradation, and 5 compounds showed improvement of activity compared to the known VIF inhibitor VEC-5 (1) with IC $$_{50 }$$ values about 20 $$μ $$ M. The findings described here will be useful for the development of more potent VIF inhibitors.
Starting Page	221
Ending Page	243
Page Count	23
File Format	PDF
ISSN	13811991
Journal	Molecular Diversity
Volume Number	17
Issue Number	2
e-ISSN	1573501X
Language	English
Publisher	Springer Netherlands
Publisher Date	2013-02-03
Publisher Place	Dordrecht
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	VIF–ElonginC interaction inhibition VEC-5 Anti-HIV-1 Indolizine derivatives Structure-activity relationship Biochemistry Organic Chemistry Polymer Sciences Pharmacy
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Medicine Drug Discovery Molecular Biology Physical and Theoretical Chemistry Information Systems Catalysis Inorganic Chemistry

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4	Project PI / Joint PI	Principal Investigator and Joint Principal Investigators of the project	Dr. B. Sutradhar bsutra@ndl.gov.in Prof. Saswat Chakrabarti will be added soon
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