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Quinoxaline chemistry: Part 10: Quinoxaline 10-oxa-analogues of trimetrexate (TMQ ) and of 5,8-dideazafolic acid: synthesis and evaluation of in vitro anticancer activity

Vitale, Gabriella and Corona, Paola and Loriga, Mario and Paglietti, Giuseppe (1998) Quinoxaline chemistry: Part 10: Quinoxaline 10-oxa-analogues of trimetrexate (TMQ ) and of 5,8-dideazafolic acid: synthesis and evaluation of in vitro anticancer activity. Il Farmaco, Vol. 53 (2), p. 150-159. ISSN 0014-827X. Article.

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DOI: 10.1016/S0014-827X(98)00003-2

Abstract

Among twenty-eight novel compounds (twenty-two 2,3-disubstituted-6-[(substituted-phenoxy)methyl-quinoxalines and six 4-[(2,3-disubstituted-quinoxalin-6-yl methoxylbenzoylglutamates) only thirteen were selected at NO for evaluation of their in vitro anticancer activity. The results have shown that compounds 31,c,b,e and 4b were endowed with significantly high values of percent tumor growth inhibition on several tumor cell lines at 10−4 M, while compound 3t was characterized by a high selectivity, being still strongly inhibiting on three cell lines at 105 M. Comparison of the presently observed activity with that of the previously described aza-analogues confirms that the effected isosteric substitution is highly valuable in some cases.

Item Type:Article
ID Code:572
Status:Published
Refereed:Yes
Uncontrolled Keywords:Anticancer agents, quinoxaline derivatives, trimetrexate analogues, 5,8-dideazafolic acid analogues
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
Publisher:Elsevier
ISSN:0014-827X
Deposited On:18 Aug 2009 10:02

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