Evidence map›Paper›PMID 22978745›Full record

ArticleJournal of medicinal chemistry2012

Anti-AIDS agents 90. novel C-28 modified bevirimat analogues as potent HIV maturation inhibitors.

Keduo Qian, Ibrahim D Bori, Chin-Ho Chen, Li Huang, Kuo-Hsiung Lee

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.

0numbers the graph read from it
0cells of the map it votes in
24citing papers in PubMed
2.9field-weighted citation impact, top 9% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

24 citing papers in PubMed, 56 citations in OpenAlex.

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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

5 authors at 3 institutions in 2 countries.

Keduo QianNatural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, North Carolina 27599, USA. kdqian@unc.edu
Ibrahim D Bori
Chin-Ho Chen
Li Huang
Kuo-Hsiung Lee
Duke Medical Center · USUniversity of North Carolina at Chapel Hill · USChina Medical University · TW

Funding

Modified Triterpines as Potent HIV Fusion InhibitorsR01AI077417 · NIAID · UNIV OF NORTH CAROLINA CHAPEL HILL · PI LEE, KUO-HSIUNG · 2008 to 2012
$2.4M
NIAID NIH HHS AI-077417NIAID NIH HHS R01 AI077417
6 · The paper itself

Abstract

In a continuing study of bevirimat (2), the anti-HIV-maturation clinical trials agent, 28 new betulinic acid (BA, 1) derivatives were designed and synthesized. Among these compounds, 17, with a C-28 MEM ester moiety, and 22, with a C-28 ethyl hexanoate, increased the anti-HIV replication activity compared with 2 by 2-fold while compounds 40, 41, 48, and 49, with C-28 piperazine or piperidine amide substitutions, increased the activity by 3- to 15-fold. The best new compound, 41, exhibited an anti-HIV IC(50) of 0.0059 μM compared with 0.087 μM for 2. All of the active compounds showed only antimaturation effects, as confirmed by TZM-bl assay, in blocking the HIV replication. The results suggest that proper C-28 substitutions can further enhance the antimaturation activity of 2 without any antientry effects. Thus, 41 may serve as a promising new lead for development of anti-AIDS clinical trial candidates.

Indexed as

Anti-HIV AgentsCell LineDrug DesignDrug StabilityHIV-1HumansPentacyclic TriterpenesStructure-Activity RelationshipSuccinatesTriterpenesVirus ReplicationAnti-HIV AgentsbevirimatPentacyclic TriterpenesSuccinatesTriterpenes

Identifiers

PMID22978745
PMCPMC3478670
OpenAlexW2018697541

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.