一类新型抗肿瘤剂。I. 化学与动物实验。

A novel class of antitumour agents. I. Chemistry and animal experiments.

作者信息

Savage D S, Emminger A, Mohr U

机构信息

Scientific Development Group, Organon, Newhouse, Lanarkshire, Scotland.

出版信息

Cancer Lett. 1977 Mar;2(4-5):267-72. doi: 10.1016/s0304-3835(77)80031-1.

DOI:10.1016/s0304-3835(77)80031-1

PMID:45729

Abstract

Newly synthesized tertiary amino steroids, among them 2 beta,16 beta-dipiperidino-5 alpha-androstane-3 alpha,17 beta-diol dipivalate (DAP), were tested in three animal species as to their antitumour activity against transplantable tumours. The acute toxicity of DAP was similar to that of cyclophosphamide and considerably lower than vinblastine. Rats with Walker ascites, treated intraperitoneally with DAP, survived up to one year without ascites; untreated animals died within 10 days of transplantation. Intragastric and intraperitoneal application of DAP caused side effects suggesting a local toxicity.

摘要

新合成的叔胺类甾体化合物，其中包括2β,16β - 二哌啶基 - 5α - 雄甾烷 - 3α,17β - 二醇二特戊酸酯（DAP），在三种动物物种中针对可移植肿瘤进行了抗肿瘤活性测试。DAP的急性毒性与环磷酰胺相似，且远低于长春碱。用DAP腹腔注射治疗的Walker腹水大鼠可存活长达一年且无腹水；未治疗的动物在移植后10天内死亡。DAP的胃内和腹腔内给药引起了提示局部毒性的副作用。