150840-27-0Relevant articles and documents
Betulinic acid derivatives as human immunodeficiency virus type 2 (HIV-2) inhibitors
Dang, Zhao,Lai, Weihong,Qian, Keduo,Ho, Phong,Lee, Kuo-Hsiung,Chen, Chin-Ho,Huang, Li
experimental part, p. 7887 - 7891 (2010/04/30)
Wepreviously reported that [[N-[3β-hydroxyllup-20(29)-en-28-oyl]-7- aminoheptyl]carbamoyl]methane (A43D, 4) was a potent HIV-1 entry inhibitor. However, 4 was inactive against HIV-2 virus, suggesting the structural requirements for targeting these two ret
Betulinic acid derivatives: A new class of specific inhibitors of human immunodeficiency virus type 1 entry
Soler, Fran?oise,Poujade, Christèle,Evers, Michel,Carry, Jean-Christophe,Hénin, Yvette,Bousseau, Anne,Huet, Thierry,Pauwels, Rudi,De Clercq, Erik,Mayaux, Jean-Fran?ois,Le Pecq, Jean-Bernard,Dereu, Norbert
, p. 1069 - 1083 (2007/10/03)
A novel series of ω-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 ω-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.
Lupane derivatives, their preparation and the pharmaceutical compositions which contain them
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, (2008/06/13)
The present invention relates to new lupane dervivatives of the general formula: STR1 to their salts, to their preparation and to the pharmaceutical compositions which contain them.