精胍菌素类似物的合成与抗肿瘤活性。I. 7-胍基-3-羟基酰基部分的化学修饰。

Synthesis and antitumor activity of spergualin analogues. I. Chemical modification of 7-guanidino-3-hydroxyacyl moiety.

作者信息

Umeda Y, Moriguchi M, Kuroda H, Nakamura T, Iinuma H, Takeuchi T, Umezawa H

出版信息

J Antibiot (Tokyo). 1985 Jul;38(7):886-98. doi: 10.7164/antibiotics.38.886.

DOI:10.7164/antibiotics.38.886

Abstract

Many analogues and derivatives of an antitumor antibiotic, spergualin, were synthesized, and the relationships between the structure and the activity against mouse L-1210 tumor were studied. Both modification of the 15-hydroxyl group and alteration of chain-length of the omega-guanidinoacyl moiety affected the activity. 15-Deoxyspergualin (18, 1-amino-19-guanidino-11-hydroxy-4,9,12-triazanonadecane-10,13-d ion e) and its analogue 25 (1-amino-21-guanidino-11-hydroxy-4,9,12-triazauneicosane-10,13-dio ne) had strong activity, superior to that of spergualin.

摘要

合成了抗肿瘤抗生素斯佩格宁的许多类似物和衍生物，并研究了其结构与对小鼠L-1210肿瘤活性之间的关系。15-羟基的修饰和ω-胍基酰基部分链长的改变均影响活性。15-脱氧斯佩格宁（18, 1-氨基-19-胍基-11-羟基-4,9,12-三氮杂十九烷-10,13-二酮）及其类似物25（1-氨基-21-胍基-11-羟基-4,9,12-三氮杂二十一烷-10,13-二酮）具有很强的活性，优于斯佩格宁。