Bereich Organische Chemie, Martin-Luther-Universität Halle-Wittenberg, Kurt-Mothes-Str 2, D-06120 Halle, Saale, Germany.
Bioorg Med Chem. 2010 Feb;18(3):1344-55. doi: 10.1016/j.bmc.2009.12.024. Epub 2009 Dec 23.
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.
桦木酸醛与各种碳亲核试剂反应生成了一系列新的桦木酸衍生物，其中包括环氧化物、缩水甘油衍生物和β-羟基羰基化合物。β-羟基羰基的后续转化导致了 1,3-二酮和α,β-不饱和桦木酸衍生物的生成。这些化合物通过使用 15 个人类癌细胞系和比色 SRB 测定法进行了细胞毒性测试。一些化合物显示出显著的抗肿瘤活性。
