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7-烷氧基米托蒽醌类化合物的合成及其生物活性

Synthesis and biological activities of 7-alkoxymitosanes.

作者信息

Urakawa C, Nakano K, Imai R

出版信息

J Antibiot (Tokyo). 1980 Aug;33(8):804-9. doi: 10.7164/antibiotics.33.804.

DOI:10.7164/antibiotics.33.804
PMID:7429982
Abstract

A facile alcoholysis of 7-methoxymitosanes and 5-methoxyindolequinone under basic conditions was discovered and a series of 7-alkoxymitosanes were synthesized from mitomycins A and B using this reaction. They showed strong antibacterial activity against various Gram-positive and Gram-negative bacteria and were potent inhibitors of cultivating HeLa S-3 cells in vitro. Among them, 7-n-propoxy-7-demethoxymitomycin A (2) showed the strongest antitumor activity against solid type Sarcoma-180 in mice.

摘要

我们发现了在碱性条件下7-甲氧基丝裂霉素和5-甲氧基吲哚醌的一种简便醇解反应,并利用该反应从丝裂霉素A和B合成了一系列7-烷氧基丝裂霉素。它们对多种革兰氏阳性菌和革兰氏阴性菌均表现出较强的抗菌活性,并且是体外培养HeLa S-3细胞的有效抑制剂。其中,7-正丙氧基-7-去甲氧基丝裂霉素A(2)对小鼠实体型肉瘤-180显示出最强的抗肿瘤活性。

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