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Syntheses and biological activities of rebeccamycin analogues with uncommon sugars.

Abstract：

:Rebeccamycin analogues containing uncommon sugars and substitutions on the imide nitrogen have been synthesized. Their cytotoxicities were tested in colon cancer and leukemia cells. Their ability to target topoisomerase I was examined using the in vivo complex of the topoisomerase bioassay in Hela cells. Compared with aglycon 1, the modified compounds with various sugar moieties showed more potent cytotoxicities and topo I targeting ability. In addition, the rebeccamycin analogues with various uncommon sugars showed distinct cytotoxicities and topo I targeting activities. The activity of compounds with 2-deoxyglucose (8 and 9) > compounds with 2,6-deoxyglucose (5 and 6) > compounds with 2,3,6-deoxyglucose (10). Furthermore, the anticancer activity of compounds correlated with their ability to target endogenous topo I. These results suggest that the sugar moiety, especially the 2-OH and 6-OH group of the sugar, rather than the modifications in imide structure on the indolocarbazole ring, is a key element for its activity.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Zhang G,Shen J,Cheng H,Zhu L,Fang L,Luo S,Muller MT,Lee GE,Wei L,Du Y,Sun D,Wang PG

doi

10.1021/jm0493764

keywords:

subject

Has Abstract

pub_date

2005-04-07 00:00:00

pages

2600-11

issue

7

eissn

0022-2623

issn

1520-4804

journal_volume

48

pub_type

杂志文章

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