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New carbocyclic analogues of netropsin: synthesis and inhibition of topoisomerases

100%

Puckowska A., Bielawski K., Bielawska A., Rozanski A.

Acta Biochimica Polonica

2002

tom 49

nr 1

A series of carbocyclic analogues of netropsin were synthesized and evaluated for their capacity to inhibit human topoisomerases I and II in vitro. The compounds are oligopeptides containing 1,4-di- and 1,2,5-trisubstituted benzene rings and unsubstituted N-terminal NH2 groups. Compounds 4-7 consist of two netropsin-like units linked by aliphatic (tetra- and hexamethylene) chains. In the topoisomerase I and II assay, the relaxation of pBR322 plasmid was inhibited by compounds 4-7 at 100 uM concentration.

Synthetic analogues of netropsin and distamycin-synthesis of a new pyridine and carbocyclic analogues of the pyrrolecarboxamide antitumour antibiotics

76%

Bartulewicz D., Bielawski K., Markowska A., Zwierz K., Puckowska A., Rozanski A.

Acta Biochimica Polonica

1998

tom 45

nr 1

A new series of pyridine-containing analogues III-XXII of distamycin A and netropsin was investigated by the molecular mechanics technique and molecular modelling. A pyridine analogue of netropsin (VII) is described, the first compound based on molecular studies, and two carbocyclic analogues of distamycin A with an N-terminal chloro- or bromoacetyl group (VIa, VIIa) were synthesized, as well as carbocyclic analogues of netropsin (VIIIb, Xb), potential carriers of alkylating elements. The potential use of VIa, VII, VIIa, VIIIb and Xb as carriers to place into the minor groove of DNA chemical groups capable of modifying DNA, is discussed.

Ograniczanie wyników

2 Acta Biochimica Polonica

2 Bielawski K.

2 Puckowska A.

2 Rozanski A.

1 Bartulewicz D.

1 Bielawska A.

1 Markowska A.

1 Zwierz K.

1 2002

1 1998

Wyniki wyszukiwania

New carbocyclic analogues of netropsin: synthesis and inhibition of topoisomerases

Synthetic analogues of netropsin and distamycin-synthesis of a new pyridine and carbocyclic analogues of the pyrrolecarboxamide antitumour antibiotics