Synthesis and in vitro antitumor activity of multi-methoxyl carbazole analogues.
- Author:
Fu-min ZHAI
1
;
Qi-dong YOU
;
Hua WANG
;
Xiao-guang CHEN
;
Yan LI
;
Hong-yan LI
Author Information
- Publication Type:Journal Article
- MeSH: Antineoplastic Agents; chemical synthesis; chemistry; pharmacology; Carbazoles; chemical synthesis; chemistry; pharmacology; HT29 Cells; drug effects; Humans; KB Cells; drug effects; Molecular Structure
- From: Acta Pharmaceutica Sinica 2004;39(10):808-812
- CountryChina
- Language:Chinese
-
Abstract:
AIMTo design and synthesize new methoxyl carbazole analogues as antitumor compounds.
METHODSMethoxyl-nitrobiphenyls (3a-3c) were prepared through the Ullmann reaction of 4,5-dimethoxyl-2-bromonitrobenzene and methoxyl-iodobenzene compounds with the catalysis of copper powder, and then reduced by P(EtO)3 to obtain methoxyl carbazoles 4a-4c. The modification at 9-position of the methoxyl carbazoles (4a-4c) gives 16 carbazole derivatives (5a-5p). These compounds were confirmed by 1HNMR, MS, IR and elemental analysis.
RESULTIn vitro antitumor activities evaluation in vitro demonstrated that IC50 value of the target compounds 4c, 5a, 5b, 5g, 5h, 5i, 5l, 5n and 5p against HT-29 cells were 12.1, 10.6, 8.1, 3.1, 4.4, 10.1 and 9.2 micromol x L(-1) respectively, and IC50 value of the target compound 4a against KB was 17.7 micromol x L(-1).
CONCLUSIONSome of the target compounds have better inhibitory effects against H-29 and KB cells.
