Some benzoxazoles and benzimidazoles as DNA topoisomerase I and II inhibitors

被引：21

作者：

Oksuzoglu, Emine ^{[2
]}

Tekiner-Gulbas, Betul ^{[1
]}

Alper, Sabiha ^{[1
]}

Temiz-Arpaci, Ozlem ^{[1
]}

Ertan, Tugba ^{[1
]}

Yildiz, Ilkay ^{[1
]}

Diril, Nuran ^{[2
]}

Sener-Aki, Esin ^{[1
]}

Yalcin, Ismail ^{[1
]}

机构：

[1] Hacettepe Univ, Fac Pharm, Dept Pharmaceut Chem, TR-06100 Ankara, Turkey

[2] Hacettepe Univ, Fac Sci, Dept Mol Biol, TR-06532 Ankara, Turkey

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2008年 / 23卷 / 01期

关键词：

DNA topoisomerase I; topoisomerase II; inhibition; benzoxazoles; benzimidazoles;

D O I：

10.1080/14756360701342516

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Some novel fused heterocyclic compounds of 2, 5-disubstituted-benzoxazole and benzimidazole derivatives, which were previously synthesized by our group, were investigated for their inhibitory activity on both eukaryotic DNA topoisomerase I and II in a cell free system. 2-Phenoxymethylbenzimidazole (17), 5-amino-2-(p-fluorophenyl)benzoxazole (3), 5-amino-2-(p-bromophenyl)benzoxazole (5), 5-nitro-2-phenoxymethyl-benzimidazole (18), 2-(p-chlorobenzyl)benzoxazole (10) and 5-amino-2-phenylbenzoxazole (2) were found to be more potent as eukaryotic DNA topoisomerase I poisons than the reference drug camptothecin having IC50 values of 14.1, 132.3, 134.1, 248, 443.5, and 495M, respectively. 5-Chloro-2-(p-methylphenyl)benzoxazole (4), 2-(p-nitrobenzyl)benzoxazole (6) and 5-nitro-2-(p-nitrobenzyl)benzoxazole (8) exhibited significant activity as eukaryotic DNA topoisomerase II inhibitors, having IC50 values of 22.3, 17.4, 91.41M, respectively, showing higher potency than the reference drug etoposide.

引用

页码：37 / 42

页数：6

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