SYNTHESIS AND ACTIVITY OF BREFELDIN-A ANALOGS AS INDUCERS OF CANCER CELL-DIFFERENTIATION AND APOPTOSIS

Authors
ZHU JW HORI H NOJIRI H TSUKUDA T TAIRA Z
Citation
Jw. Zhu et al., SYNTHESIS AND ACTIVITY OF BREFELDIN-A ANALOGS AS INDUCERS OF CANCER CELL-DIFFERENTIATION AND APOPTOSIS, Bioorganic & medicinal chemistry letters, 7(2), 1997, pp. 139-144
Citations number
9
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
2
Year of publication
1997
Pages
139 - 144
Database
ISI
SICI code
0960-894X(1997)7:2<139:SAAOBA>2.0.ZU;2-H
Abstract
We designed and synthesized several brefeldin A (BFA) analogs. These c ompounds were evaluated for the ability to induce differentiation and apoptosis in human colonic carcinoma cell line HCT116. Diacetyl BFA (2 a), 4-acetyl BFA (2b), 7-acetyl BFA (2c), and 10,11-epoxy BFA (3b) wer e active but tetrahydro BFA (3a) and other analogs could not induce th e malignant cells to differentiate. The results suggested that the moi ety from 1- to 4-position in BFA as well as its conformational rigidit y is essential for its biological activity. (C) 1997, Elsevier Science Ltd.