Betulinic acid derivatives: a new class of human immunodeficiency virus type 1 specific inhibitors with a new mode of action.

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.

[Preparation and experimental antitumor activity of a new semi-synthetic antibiotic: 14-diethoxyacetoxy daunorubicin (R.P. 33 921)]. / Préparation et activité antitumorale expérimentale d'un nouvel antibiotique semi-synthétique : la diéthoxyacétoxy-14 daunorubicine (33 921 R.P,).

14-diethoxyacetoxy daunorubicin (R.P. 33 921) was chosen among a series of new daunorubicin analogues. Its preparation from daunorubicin and its biological activities are described. It displays an antitumoral activity in mice with a better chemotherapeutic index than daunorubicin and doxorubicin.