蔗糖亚硝基脲衍生物作为中枢神经系统抗癌剂的合成。

Synthesis of nitrosourea derivatives of sucrose as central nervous system anticancer agents.

作者信息

Almquist R G, Reist E J

出版信息

J Med Chem. 1977 Oct;20(10):1246-50. doi: 10.1021/jm00220a004.

Abstract

Nitrosourea derivatives of sucrose have been synthesized for the purpose of obtaining anticancer agents with activity against brain cancer. Two such compounds, 6,6'-dideoxy-6,6'-di(3-methyl-3-nitrosoureido) sucrose (13) and 1', 6,6'-trideoxy-1',6,6-tri(3-methyl-3-nitrosoureido) sucrose (14), and their respective acetylated derivatives 15 and 16 have been prepared from sucrose. Compounds 13 and 14 have demonstrated antitumor activity against both L1210 leukemia and ependymoblastoma brain tumor in mice.

摘要

为了获得对脑癌具有活性的抗癌剂，已合成了蔗糖的亚硝基脲衍生物。已从蔗糖制备了两种这样的化合物，即6,6'-二脱氧-6,6'-二(3-甲基-3-亚硝基脲基)蔗糖(13)和1',6,6'-三脱氧-1',6,6-三(3-甲基-3-亚硝基脲基)蔗糖(14)，以及它们各自的乙酰化衍生物15和16。化合物13和14已在小鼠中显示出对L1210白血病和室管膜母细胞瘤脑肿瘤的抗肿瘤活性。