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[柔红霉素和洋红霉素14-取代衍生物的毒性及抗肿瘤活性研究]

[Study of toxicity and antineoplastic activity of 14-substituted derivatives of rubomycin and carminomycin].

作者信息

Ul'ianova L A, Iudina O I, Tarasova V E, Shepelevtseva N G, Olsuf'eva E N, Povarov L S, Gol'dberg L E

出版信息

Antibiot Khimioter. 1990 Feb;35(2):24-6.

PMID:2088341
Abstract

Toxicity and antitumor activity of five derivatives of rubomycin and carminomycin were studied in animals. The derivatives were prepared by modification of the methyl C-14 group. These were the following: 14-chlorrubomycin, 14-chlorcarminomycin, 14-salicyloyloxyrubomycin, 14-salicyloyloxycarminomycin and 14-quinaldinoyloxyrubomycin. The chemotherapeutic study revealed that, in their activity, all the compounds were inferior to the starting antibiotics. Unlike the other derivatives, 14-chlorcarminomycin induced a significant inhibition of leukemia P-388 development (the average lifespan of the mice amounted to 165 per cent as compared to the control). However, in the magnitude of its effect, the derivative was inferior to carminomycin.

摘要

对柔红霉素和洋红霉素的五种衍生物的毒性和抗肿瘤活性进行了动物研究。这些衍生物是通过对甲基C-14基团进行修饰制备的。它们如下:14-氯柔红霉素、14-氯洋红霉素、14-水杨酰氧基柔红霉素、14-水杨酰氧基洋红霉素和14-喹哪啶酰氧基柔红霉素。化疗研究表明,所有化合物的活性均低于起始抗生素。与其他衍生物不同,14-氯洋红霉素对白血病P-388的发展有显著抑制作用(与对照组相比,小鼠的平均寿命达到165%)。然而,该衍生物在作用强度上低于洋红霉素。

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