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Quinoxaline chemistry: Part 11: 3-Phenyl-2 [phenoxy- and phenoxymethyl]-6(7) or 6,8-substituted quinoxalines and N-[4-(6(7)-substituted or 6,8-disubstituted-3-phenylquinoxalin-2-yl)hydroxy or hydroxymethyl]benzoylglutamates: synthesis and evaluation of in vitro anticancer activity and enzymatic inhibitory activity against dihydrofolate reductase and thymidylate synthase

Loriga, Mario and Vitale, Gabriella and Paglietti, Giuseppe and Corona, Paola and Costi, Maria Paola (1998) Quinoxaline chemistry: Part 11: 3-Phenyl-2 [phenoxy- and phenoxymethyl]-6(7) or 6,8-substituted quinoxalines and N-[4-(6(7)-substituted or 6,8-disubstituted-3-phenylquinoxalin-2-yl)hydroxy or hydroxymethyl]benzoylglutamates: synthesis and evaluation of in vitro anticancer activity and enzymatic inhibitory activity against dihydrofolate reductase and thymidylate synthase. Il Farmaco, Vol. 53 (7), p. 480-493. ISSN 0014-827X. Article.

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DOI: 10.1016/S0014-827X(98)00054-8

Abstract

Twenty-four out of twenty-nine quinoxalines were selected at the National Cancer Institute, Bethesda, Md, USA, for in vitro anticancer screening. Among these, 10 derivatives exhibited high values of percent tumor growth inhibition at a concentration of 10−4 M in all cancer cell lines. Four of these compounds maintained these values at 10−5 M, whereas a certain number exhibited significant values of percent inhibition at the most diluted concentrations (10−8 – 10−6 M). Inhibitory activity against dihydrofolate reductase (DHFR) (bovine and rat liver) was determined for the most active compounds. This test showed that this type of quinoxaline exhibited an appreciable activity in comparison with the previously described aza analogues. In the other test (Lactobacillus casei, thymidylate synthase (TS), human HTS) no or poor activity was detected in both series of compounds.

Item Type:Article
ID Code:1391
Status:Published
Refereed:Yes
Uncontrolled Keywords:Antifolate agents, anticancer agents, enzyme inhibition, dihydrofolate reductase
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
Publisher:Elsevier
ISSN:0014-827X
Additional Information:Pubblicato online il 10 febbraio 1999.
Deposited On:18 Aug 2009 10:05

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