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

• Authors: Danuta Bartulewicz , Agnieszka Markowska , Sławomir Wołczyński , Milena Dąbrowska , Andrzej Różański
• Languages of publication: EN

Abstracts

EN

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.

Keywords

EN

lexitropsin; carbocyclic analogues of distamycin and netropsin; molecular modelling

• Publisher: Polish Biochemical Society
• Journal: Acta Biochimica Polonica
• Year: 2000
• Volume: 47
• Issue: 1
• Pages: 23-35

Dates

published

2000

received

1999-10-25

Contributors

author

Danuta Bartulewicz

• Department of Organic Chemistry, Medical Academy of Białystok, Białystok, Poland

author

Agnieszka Markowska

• Department of Organic Chemistry, Medical Academy of Białystok, Białystok, Poland

author

Sławomir Wołczyński

• Department of Gynaecological Endocrinology, Medical Academy of Białystok, Białystok, Poland

author

Milena Dąbrowska

• Department of Haematological Diagnostics, Medical Academy of Białystok, Białystok, Poland

author

Andrzej Różański

• Department of Organic Chemistry, Medical Academy of Białystok, Białystok, Poland

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