Publication Date:
2006
Short description:
Novel 3-benzoyl-2-piperazinylquinoxaline derivatives as potential antitumor agents / Piras, S., Loriga, M., Carta, A., Paglietti, G., Costi, M.P., Ferrari, S.. - In: JOURNAL OF HETEROCYCLIC CHEMISTRY. - ISSN 0022-152X. - 43:(2006), pp. 541-548. [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.
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.
Iris type:
1.1 Articolo in rivista
Keywords:
IN-VITRO ANTICANCER; CLASSICAL ANTIFOLATE AGENTS; QUINOXALINE CHEMISTRY
List of contributors:
Piras, Sandra; Loriga, M; Carta, Antonio; Paglietti, G; Costi, M. P.; Ferrari, S.
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