New carbocyclic analogues of netropsin: synthesis and inhibition of topoisomerases.
作者信息
Pućkowska Anna, Bielawski Krzysztof, Bielawska Anna, Rózański Andrzej
机构信息
Department of Organic Chemistry, Medical Academy of Bialystok, Poland.
出版信息
Acta Biochim Pol. 2002;49(1):177-83.
PMID:12136938
Abstract
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 microM concentration.
摘要
相似文献
1
New carbocyclic analogues of netropsin: synthesis and inhibition of topoisomerases.
Acta Biochim Pol. 2002;49(1):177-83.
2
Carbocyclic analogues of netropsin and distamycin: DNA-binding properties and inhibition of DNA topoisomerases.
Arch Pharm (Weinheim). 2002 Nov;335(9):422-6. doi: 10.1002/1521-4184(200212)335:9<422::AID-ARDP422>3.0.CO;2-5.
3
New carbocyclic lexitropsins with dinitromustard as N-terminal fragment. Inhibition of topoisomerases.
Acta Pol Pharm. 2003 Mar-Apr;60(2):119-21.
4
Aromatic analogues of DNA minor groove binders--synthesis and biological evaluation.
Eur J Med Chem. 2004 Jan;39(1):99-105. doi: 10.1016/j.ejmech.2003.11.005.
5
Synthetic analogues of netropsin and distamycin. V. Synthesis of a carbocyclic bis-lexitropsin as potential DNA cleaving agent.
Rocz Akad Med Bialymst. 1999;44:200-15.
6
7
Synthetic analogues of netropsin and distamycin. VI. Synthesis of carbocyclic lexitropsins containing a bioreductive element.
Acta Pol Pharm. 2000 Nov;57 Suppl:71-6.
8
Design, synthesis and biological evaluation of new oligopyrrole carboxamides linked with tricyclic DNA-intercalators as potential DNA ligands or topoisomerase inhibitors.
Eur J Med Chem. 2007 Jun;42(6):752-71. doi: 10.1016/j.ejmech.2006.12.039. Epub 2007 Mar 2.
9
Carbocyclic analogues of lexitropsin--DNA affinity and endonuclease inhibition.
Acta Pol Pharm. 2007 Mar-Apr;64(2):115-9.
10
Synthetic analogues of netropsin and distamycin. II. Synthesis of a carbocyclic analogue of the pyrrolecarboxamide antitumour antibiotics.
Rocz Akad Med Bialymst. 1995;40(2):364-75.
Zotero 插件