水溶性多卡霉素B1前药的合成及其抗肿瘤活性
Synthesis and antitumor activity of water-soluble duocarmycin B1 prodrugs.
作者信息
Asai A, Nagamura S, Kobayashi E, Gomi K, Saito H
机构信息
Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Japan.
出版信息
Bioorg Med Chem Lett. 1999 Oct 18;9(20):2995-8. doi: 10.1016/s0960-894x(99)00518-1.
Abstract
The water-soluble duocarmycin B1 prodrugs such as glycoside 3, phosphate 4 and carbamate 5 were synthesized for improving biological and pharmaceutical profiles of duocarmycin. Among these prodrugs, N-methylpiperazinylcarbamoyl derivative 5 exhibited potent antitumor activity against several human tumors in vivo.
摘要
为改善多卡霉素的生物学和药学性质，合成了水溶性多卡霉素B1前药，如糖苷3、磷酸盐4和氨基甲酸酯5。在这些前药中，N-甲基哌嗪基氨基甲酰基衍生物5在体内对几种人类肿瘤表现出强大的抗肿瘤活性。
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