期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 36, 期 5, 页码 461-467出版社
EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/S0223-5234(01)01232-6
关键词
netropsin; distamycin; carbocyclic analogues of distamycin
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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