150840-32-7Relevant articles and documents
Synthesis and anti-HIV activity of bi-functional betulinic acid derivatives
Huang, Li,Ho, Phong,Lee, Kuo-Hsiung,Chen, Chin-Ho
, p. 2279 - 2289 (2007/10/03)
Betulinic acid (BA) derivatives with a side chain at C-3 can inhibit HIV-1 maturation. On the other hand, BA derivatives with a side chain at C-28 can block HIV-1 entry. In order to combine the anti-maturation and anti-entry activities in a single molecul
Anti-AIDS agents 49. Synthesis, anti-HIV, and anti-fusion activities of IC9564 analogues based on betulinic acid
Sun, I-Chen,Chen, Chin-Ho,Kashiwada, Yoshiki,Wu, Jiu-Hong,Wang, Hui-Kang,Lee, Kuo-Hsiung
, p. 4271 - 4275 (2007/10/03)
The betulinic acid derivative IC9564 inhibits human immunodeficiency virus (HIV)-1 entry. Among a series of IC9564 derivatives, 5 and 20 were the most promising compounds against HIV infection with EC50 values of 0.33 and 0.46 μM, respectively.
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.