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

✍ Scribed by Sandra Piras; Mario Loriga; Antonio Carta; Giuseppe Paglietti; M. Paola Costi; Stefania Ferrari

Publisher
Journal of Heterocyclic Chemistry
Year
2006
Tongue
English
Weight
202 KB
Volume
43
Category
Article
ISSN
0022-152X

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✦ Synopsis

Abstract

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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 (K~i~) values in the range of 0.6‐70 μM. Compounds 21, 23, 24 showed K~i~ in the range of 10‐38 μM against both hDHFR and hTS.

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