| Title |
Design, synthesis and biological evaluation of indolizine derivatives as HIV-1 VIF–ElonginC interaction inhibitors
|
|---|---|
| Published in |
Molecular Diversity, February 2013
|
| DOI | 10.1007/s11030-013-9424-3 |
| Pubmed ID | |
| Authors |
Wenlin Huang, Tao Zuo, Hongwei Jin, Zhenming Liu, Zhenjun Yang, Xianghui Yu, Liangren Zhang, Lihe Zhang |
| 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 μM. The findings described here will be useful for the development of more potent VIF inhibitors. |
X Demographics
The data shown below were collected from the profile of 1 X user who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| United States | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 30 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 30 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 5 | 17% |
| Student > Doctoral Student | 4 | 13% |
| Student > Master | 4 | 13% |
| Researcher | 4 | 13% |
| Student > Bachelor | 3 | 10% |
| Other | 3 | 10% |
| Unknown | 7 | 23% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 14 | 47% |
| Biochemistry, Genetics and Molecular Biology | 4 | 13% |
| Agricultural and Biological Sciences | 1 | 3% |
| Pharmacology, Toxicology and Pharmaceutical Science | 1 | 3% |
| Unknown | 10 | 33% |
Attention Score in Context
This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 05 February 2013.
All research outputs
#18,327,422
of 22,694,633 outputs
Outputs from Molecular Diversity
#323
of 460 outputs
Outputs of similar age
#219,516
of 283,119 outputs
Outputs of similar age from Molecular Diversity
#2
of 3 outputs
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