title: Synthesis and biological evaluation of antitumour-active betulin derivatives.
abstract: The reaction of betulinic aldehydes with various carbon nucleophiles gave a series of new betulin derivatives, among them epoxides, glycidic derivatives and beta-hydroxy carbonyl compounds. Subsequent transformations of the beta-hydroxy carbonyls lead to 1,3-diketo- and alpha,beta-unsaturated betulin derivatives. These compounds were assayed for cytotoxicity using 15 human cancer cell lines and a colorimetric SRB-assay. Several compounds revealed significant antitumour activity.
authors.affiliation: Bereich Organische Chemie, Martin-Luther-Universität Halle-Wittenberg, Kurt-Mothes-Str 2, D-06120 Halle, Saale, Germany. rene.csuk@chemie.uni-halle.de
authors.forename: René
authors.initials: R
authors.lastname: Csuk
authors.forename: Alexander
authors.initials: A
authors.lastname: Barthel
authors.forename: Ralph
authors.initials: R
authors.lastname: Kluge
authors.forename: Dieter
authors.initials: D
authors.lastname: Ströhl
authors.forename: Harish
authors.initials: H
authors.lastname: Kommera
authors.forename: Reinhard
authors.initials: R
authors.lastname: Paschke
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy*; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000138:chemical synthesis* / Q000494:pharmacology*; D000094062:Betulinic Acid
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D014315:Triterpenes; C002503:betulin; D000094062:Betulinic Acid