[Synthesis and antitumor activity of betulin, erythrodiol and uvaol aminopropoxy derivatives].

Autor: Kazakova OB, Giniiatullina GV, Tolstikov GA, Baĭkova IP, Zaprutko L, Apryshko GN
Jazyk: ruština
Zdroj: Bioorganicheskaia khimiia [Bioorg Khim] 2011 May-Jun; Vol. 37 (3), pp. 414-24.
DOI: 10.1134/s1068162011030101
Abstrakt: The synthesis of aminopropoxy derivatives of betulin, erythrodiol, uvaol and oleantriol via cyanoethylation of triterpenoids hydroxyl groups and subsequent reduction of cyanoethyl fragments is described. High and specific in vitro antitumor activity (cytotoxicity) of 3beta,28-di-O-[3-(aminopropoxy)]lupa-20(29)-ene and 3beta-O-hydroxy-28-O-[3-(aminopropoxy)]olean-12-ene towards a wide range of human tumor cell lines is discovered. The aminopropoxy group is shown to be a new perspective pharmacophor group for design of anticancer agents on the basis of triterpenoids.
Databáze: MEDLINE