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Quinoxaline chemistry. Part 8. 2-[anilino]-3- [carboxy]-6(7)-substituted quinoxalines as non classical antifolate agents. Synthesis and evaluation of in vitro anticancer, anti-HIV and antifungal activity

Loriga, Mario and Moro, Pierangelo and Paglietti, Giuseppe and Zanetti, Stefania Anna Lucia (1997) Quinoxaline chemistry. Part 8. 2-[anilino]-3- [carboxy]-6(7)-substituted quinoxalines as non classical antifolate agents. Synthesis and evaluation of in vitro anticancer, anti-HIV and antifungal activity. Il Farmaco, Vol. 52 (8-9), p. 531-537. ISSN 0014-827X. Article.

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Abstract

Thirty quinoxalines bearing a substituted anilino group on position 2, a carboethoxy or carboxy group on position 3 and a trifluoromethyl group on position 6 or 7 of the heterocycle were prepared in order to evaluate in vitro anticancer activity. Preliminary screening performed at NCI showed that most derivatives exhibited a moderate to strong growth inhibition activity on various tumor panel cell lines between 10-5 and 10-4 molar concentrations. Interesting selectivities were also recorded between 10-8 and 10-6 M for a few compounds. One single compound exhibited good activity against Candida Albicans.

Item Type:Article
ID Code:2931
Status:Published
Refereed:Yes
Uncontrolled Keywords:Antifungal agent, quinoxaline derivatives, fluorine organic compounds
Subjects:Area 06 - Scienze mediche > MED/07 Microbiologia e microbiologia clinica
Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01 Dipartimenti > Scienze biomediche
001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
Publisher:Società chimica italiana
ISSN:0014-827X
Publisher Policy:Depositato per gentile concessione dell'Editore
Deposited On:08 Sep 2009 16:43

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