Synthesis and activity of brefeldin a analogs as inducers of cancer cell differentiation and apoptosis

被引：37

作者：

Zhu, JW

Hori, H

Nojiri, H

Tsukuda, T

Taira, Z

机构：

[1] UNIV TOKUSHIMA,DEPT BIOL SCI & TECHNOL,TOKUSHIMA 770,JAPAN

[2] TEIKYO UNIV,FAC PHARMACEUT SCI,KANAGAWA 19901,JAPAN

[3] TOKUSHIMA BUNRI UNIV,FAC PHARMACEUT SCI,YAMASHIRO,TOKUSHIMA 770,JAPAN

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(96)00588-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We designed and synthesized several brefeldin A (BFA) analogs. These compounds were evaluated for the ability to induce differentiation and apoptosis in human colonic carcinoma cell line HCT116. Diacetyl BFA (2a), 4-acetyl BFA (2b), 7-acetyl BFA (2c), and 10,11-epoxy BFA (3b) were active but tetrahydro BFA (3a) and other analogs could not induce the malignant cells to differentiate. The results suggested that the moiety from 1- to 4-position in BFA as well as its conformational rigidity is essential for its biological activity. (C) 1997, Elsevier Science Ltd.

引用

页码：139 / 144

页数：6

共 9 条

[1]

BETINA V, 1969, NEOPLASMA, V16, P23

[2] ANTI-HELA CELL EFFECT OF CYANEIN [J].