| Literature DB >> 8676341 |
M Evers1, C Poujade, F Soler, Y Ribeill, C James, Y Lelièvre, J C Gueguen, D Reisdorf, I Morize, R Pauwels, E De Clercq, Y Hénin, A Bousseau, J F Mayaux, J B Le Pecq, N Dereu.
Abstract
A series of omega-undecanoic amides of lup-20(29)-en-28-oic acid derivatives were synthesized and evaluated for activity in CEM 4 and MT-4 cell cultures against human immunodeficiency virus type 1 (HIV-1) strain IIIB/LAI. The potent HIV inhibitors which emerged, compounds 5a, 16a, and 17b, were all derivatives of betulinic acid (3beta-hydroxylup-20(29)-en-28-oic acid). No activity was found against HIV-2 strain ROD. Compound 5a showed no inhibition of HIV-1 reverse transcriptase activity with poly(C).oligo(dG) as template/primer, nor did it inhibit HIV-1 protease. Additional mechanistic studies revealed that this class of compounds interfere with HIV-1 entry in the cells at a postbinding step.Entities:
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Year: 1996 PMID： 8676341 DOI： 10.1021/jm950670t
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446