10-脱氨甲酰氧基-9-脱氢丝裂霉素B及其类似物的制备与生物活性

Preparation and biological activities of 10-decarbamoyloxy-9-dehydromitomycin B and its analogs.

作者信息

Urakawa C, Tsuchiya H, Nakano K, Nakamura N

出版信息

J Antibiot (Tokyo). 1981 Sep;34(9):1152-6. doi: 10.7164/antibiotics.34.1152.

DOI:10.7164/antibiotics.34.1152

Abstract

A new naturally occurring mitomycin, 10-decarbamoyloxy-9-dehydromitomycin B (1), was prepared by treating mitomycin B with sodium hydride. Its analogs having an exo-cyclic double bond in their structure were also synthesized. These compounds showed antibacterial and cytotoxic activities. Among them, 7-amino-10-decarbamoyloxy-9-dehydro-7-demethoxymitomycin B (2) was the most potent growth inhibitor of KB cells in vitro and, accordingly, it appears to be a potential antitumor agent.

摘要

一种新的天然存在的丝裂霉素，10-去氨甲酰氧基-9-脱氢丝裂霉素B（1），通过用氢化钠处理丝裂霉素B制备而成。还合成了其结构中具有环外双键的类似物。这些化合物表现出抗菌和细胞毒性活性。其中，7-氨基-10-去氨甲酰氧基-9-脱氢-7-去甲氧基丝裂霉素B（2）是体外对KB细胞最有效的生长抑制剂，因此，它似乎是一种潜在的抗肿瘤剂。