Design and synthesis of novel 7-aminoquinazoline derivatives: Antitumor and anticonvulsant activities

Compound 7 showed broad-spectrum antitumor activity, while compound 15 showed advanced anticonvulsant activity as well as lower toxicity than reference drugs. A novel series of 7-substituted-4(3H)-quinazolinone were designed, synthesized and evaluated for their antitumor and anticonvulsant activity....

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2012-03, Vol.22 (5), p.1879-1885
Hauptverfasser: El-Azab, Adel S., ElTahir, Kamal E.H.
Format: Artikel
Sprache:eng
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Zusammenfassung:Compound 7 showed broad-spectrum antitumor activity, while compound 15 showed advanced anticonvulsant activity as well as lower toxicity than reference drugs. A novel series of 7-substituted-4(3H)-quinazolinone were designed, synthesized and evaluated for their antitumor and anticonvulsant activity. Compound 7 revealed broad-spectrum antitumor effectiveness toward numerous cell lines that belong to different tumor subpanels, whereas compounds 9 and 18 possess selective activity toward leukemia cell lines. Additionally, compounds 3, 15, 16, 18, 19 and 20 showed advanced anticonvulsant activity as well as lower neurotoxicity than reference drugs. The achieved results proved that the distinctive compounds could be valuable as a model for future devise, acclimatization and investigation to construct more active analogues.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2012.01.071