Molecular modelling, synthesis and antitumour activity of carbocyclic analogues of netropsin and distamycin -: new carriers of alkylating elements

被引：19

作者：

Bartulewicz, D

Markowska, A

Wolczynski, S

Dabrowska, M

Rózanski, A

机构：

[1] Med Acad Bialystok, Dept Organ Chem, Bialystok, Poland

[2] Med Acad Bialystok, Dept Gynaecol Endocrinol, Bialystok, Poland

[3] Med Acad Bialystok, Dept Diagnost Haematol, Bialystok, Poland

来源：

ACTA BIOCHIMICA POLONICA | 2000年 / 47卷 / 01期

关键词：

carbocyclic analogues of distamycin and netropsin; lexitropsin; molecular modelling;

D O I：

10.18388/abp.2000_4059

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：

A series of netropsin and distamycin analogues was synthesised and investigated by molecular modelling. The lowest-energy conformations of four carbocyclic lexitropsins, potential carriers of alkylating elements, were obtained using the HyperChem 4.0 program, and compared with the DNA-lexitropsin crystal structures from the Brookhaven National Laboratory Protein Data Bank. A method for synthesis of carbocyclic lexitropsins was elaborated, with the use of a nitro group or azobenzene as precursors for the aromatic amino group. The influence of methoxy group in ortho position with respect to amide groups on the activity of the new compounds was investigated. All of the compounds tested showed high antitumour activity in the standard cell line of mammalian tumour MCF-7.

引用

页码：23 / 35

页数：13

共 38 条

[1] DESIGN AND SYNTHESIS OF ANTHRACYCLINE AND DISTAMYCIN DERIVATIVES AS NEW, SEQUENCE-SPECIFIC, DNA-BINDING PHARMACOLOGICAL AGENTS [J].