Synthesis, molecular modelling, and antiproliferative and cytotoxic effects of carbocyclic derivatives of distamycin with chlorambucil moiety

被引：27

作者：

Bartulewicz, D

Bielawski, K

Bielawska, A

Rózanski, A

机构：

[1] Med Acad Bialystok, Dept Organ Chem, PL-15230 Bialystok, Poland

[2] Med Acad Bialystok, Dept Med Chem & Drug Technol, PL-15230 Bialystok, Poland

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2001年 / 36卷 / 05期

关键词：

netropsin; distamycin; carbocyclic analogues of distamycin;

D O I：

10.1016/S0223-5234(01)01232-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New carbocylic analogues of distamycin and netropsin with chlorambucil moieties 5-8 have been synthesised. Data from the ethidium displacement assay showed that these compounds bind in the minor groove of DNA. The observed reduced affinity to AT pairs and increased affinity towards GC sequences of the carbocyclic lexitropsins with chlorambucil moiety 5-8 in comparison with netropsin and distamycin was observed and rationalised by means of molecular modelling techniques. All of the compounds 5-8 showed antiproliferative and cytotoxic effects in the standard cell line of the mammalian tumour MCF-7. (C) 2001 Editions scientifiques et medicales Elsevier SAS.

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页码：461 / 467

页数：7

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