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Novel 3-Benzoyl-2-piperazinylquinoxaline derivatives as potential antitumor agents

Piras, Sandra and Loriga, Mario and Carta, Antonio and Paglietti, Giuseppe and Costi, Maria Paola and Ferrari, Stefania (2006) Novel 3-Benzoyl-2-piperazinylquinoxaline derivatives as potential antitumor agents. Journal of Heterocyclic Chemistry, Vol. 43 (3), p. 541-548. ISSN 0022-152X. Article.

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DOI: 10.1002/jhet.5570430304

Abstract

A series of new benzoylquinoxaline derivatives (7-26) was synthesized and evaluated for antitumor activity against a panel of 60 human cell lines at the NCI of Bethesda. Among the compounds which have passed the preliminary screening, compound 23 exhibited the best profile and growth inhibition activity at 100 - 10 µM. The compounds were then tested towards a folate-dependent enzymes bio-library including Thymidylate synthases enzymes and human Dihydrofolate reductase at 10 µM. The most of compounds exhibited a moderate inhibitory activity towards all or some of the enzymes tested with detectable inhibition constants (Ki) values in the range of 0.6-70 µM. Compounds 21, 23, 24 showed Ki in the range of 10-38 µM against both hDHFR and hTS.

Item Type:Article
ID Code:2399
Status:Published
Refereed:Yes
Uncontrolled Keywords:Benzoylquinoxaline derivatives, antitumor activity, NCI
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
Publisher:Hetero Corporation
ISSN:0022-152X
Deposited On:18 Aug 2009 10:07

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