Title: Betulinic acid derivatives: a new class of specific inhibitors of human immunodeficiency virus type 1 entry
Authors: Soler, F ×
Poujade, C
Evers, M
Carry, J C
Hénin, Y
Bousseau, A
Huet, T
Pauwels, R
De Clercq, Erik
Mayaux, J F
Le Pecq, J B
Dereu, N #
Issue Date: Mar-1996
Publisher: ACS Publications
Series Title: Journal of Medicinal Chemistry vol:39 issue:5 pages:1069-83
Abstract: A novel series of omega-aminoalkanoic acid derivatives of betulinic acid were synthesized and evaluated for their activity against human immunodeficiency virus (HIV). The anti-HIV-1 activity of several members of this new series was found to be in the nanomolar range in CEM 4 and MT-4 cell cultures. The optimization of the omega-aminoalkanoic acid side chain is described. The presence of an amide function within the side chain was found important for optimal activity. RPR 103611 (14g), a statine derivative, was found to be inactive against HIV-1 protease, reverse transcriptase, and integrase as well as on gp120/CD4 binding. "Time of addition" experiments suggested interaction with an early step of HIV-1 replication. As syncytium formation, but not virus-cell binding, seems to be affected, betulinic acid derivatives are assumed to interact with the postbinding virus-cell fusion process.
ISSN: 0022-2623
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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