连氮霉素衍生物的合成及其抗肿瘤活性：C-8羟基和C-9酮基的修饰

Synthesis and antitumor activity of leinamycin derivatives: modifications of C-8 hydroxy and C-9 keto groups.

作者信息

Kanda Y, Ashizawa T, Saitoh Y, Saito H, Gomi K, Okabe M

机构信息

Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Japan.

出版信息

Bioorg Med Chem Lett. 1998 Apr 21;8(8):909-12. doi: 10.1016/s0960-894x(98)00133-4.

DOI:10.1016/s0960-894x(98)00133-4

PMID:9871510

Abstract

A series of leinamycin derivatives were synthesized and evaluated for antitumor activity. Modifications at C-8 and C-9 positions revealed a broad structure-activity relationship in vitro and some derivatives showed potent antiproliferative activity against HeLa S3 cells.

摘要

合成了一系列链黑菌素衍生物并评估其抗肿瘤活性。对C-8和C-9位的修饰揭示了体外广泛的构效关系，一些衍生物对HeLa S3细胞显示出强大的抗增殖活性。