Document Detail

Anti-AIDS agents 69. Moronic acid and other triterpene derivatives as novel potent anti-HIV agents.
MedLine Citation:
PMID:  16942019     Owner:  NLM     Status:  MEDLINE    
In a continuing structure-activity relationship study of potent anti-HIV agents, seven new triterpene derivatives were designed, synthesized, and evaluated for in vitro antiviral activity. Among them, moronic acid derivatives 19, 20, and 21 showed significant activity in HIV-1 infected H9 lymphocytes. Compounds 19 and 20 were also evaluated against HIV-1 NL4-3 and drug resistant strains in the MT-4 cell line. Compounds 19 and 20 showed better antiviral profiles than the betulinic acid analogue 8 (PA-457), which has successfully completed a Phase IIa clinical trial. Compound 20 showed potent anti-HIV activity with EC50 values of 0.0085 microM against NL4-3, 0.021 microM against PI-R (a multiple protease inhibitor resistant strain), and 0.13 microM against FHR-2 (an HIV strain resistant to 8). Promising compound 20 has become a new lead for modification, and further development of 20-related compounds as clinical trial candidates is warranted.
Donglei Yu; Yojiro Sakurai; Chin-Ho Chen; Fang-Rong Chang; Li Huang; Yoshiki Kashiwada; Kuo-Hsiung Lee
Related Documents :
22220259 - Prevention of post-transfusion hepatitis by screening of antibody to hepatitis b core a...
21654109 - Risk factors for acquiring strongyloides stercoralis infection among patients attending...
22211659 - Does gss still maintain relevance on haart outcome after the introduction of newest act...
21699699 - Antiviral drugs against hepatitis c virus.
21875269 - The need to incorporate routine cervical cancer counselling and screening in the manage...
22166559 - Serum lipids and chronic hepatitis c genotype 4: interaction and significance.
15214229 - Implants in an hiv-positive patient: a case report.
1572419 - Seroepidemiological survey of hepatitis b infection in a cohort of military recruits in...
10643719 - Subacute bacterial endocarditis with positive cytoplasmic antineutrophil cytoplasmic an...
Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural    
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  49     ISSN:  0022-2623     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2006 Sep 
Date Detail:
Created Date:  2006-08-31     Completed Date:  2006-10-16     Revised Date:  2014-09-10    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  5462-9     Citation Subset:  IM    
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Anti-HIV Agents / chemical synthesis*,  chemistry,  pharmacology
Cell Line
Drug Resistance, Viral
HIV Protease Inhibitors / pharmacology
HIV-1 / drug effects
Lymphocytes / drug effects,  virology
Oleanolic Acid / analogs & derivatives*,  chemical synthesis,  chemistry,  pharmacology
Structure-Activity Relationship
Grant Support
Reg. No./Substance:
0/Anti-HIV Agents; 0/HIV Protease Inhibitors; 6713-27-5/moronic acid; 6SMK8R7TGJ/Oleanolic Acid

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

Previous Document:  Design, synthesis, and biophysical and biological evaluation of a series of pyrrolobenzodiazepine-po...
Next Document:  Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor sel...