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Synthesis of variously substituted 3-phenoxymethyl quinoxalin-2-ones and quinoxalines capable to potentiate in vitro the antiproliferative activity of anticancer drugs in multi-drug resistant cell lines

Carta, Antonio and Loriga, Mario and Piras, Sandra and Paglietti, Giuseppe and La Colla, Paolo and Busonera, Bernardetta and Collu, Gabriella and Loddo, Roberta (2006) Synthesis of variously substituted 3-phenoxymethyl quinoxalin-2-ones and quinoxalines capable to potentiate in vitro the antiproliferative activity of anticancer drugs in multi-drug resistant cell lines. Medicinal Chemistry, Vol. 2 (2), p. 113-122. ISSN 1573-4064. Article.

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DOI: 10.2174/157340606776056197

Abstract

Two series of 1,6-dimethyl-3-phenoxymethylquinoxalin-2-ones and 1-benzyl-3-phenoxymethyl-7- trifluoromethylquinoxalin-2-ones, and a series of 2-benzyloxy-3-phenoxymethyl-7-trifluoromethylquinoxaline were synthesized. Their capability to restore/potentiate the antiproliferative activity of clinically useful drugs, such as doxorubicin (Doxo), vincristine (VCR) and etoposide (VP16), in drug-resistant human nasopharyngeal carcinoma KB cells (KBWT, KBMDR, KB7Dand KBV20C) was evaluated. In vitro data show that many quinoxalin-2-ones and quinoxalines potentiate the antiproliferative activity of Doxo and VCR in tumor-derived MDR cell lines. In this series, 17a turned out to be the most potent quinoxaline derivative in potentiating the antiproliferative activity of doxorubicin and vincristine against KBMDR and KBV20C resistant cell lines, respectively.

Item Type:Article
ID Code:534
Status:Published
Refereed:Yes
Uncontrolled Keywords:2-Quinoxalinones, quinoxalines, antiproliferative activity, multidrug resistance, P-glycoprotein inhibitors, doxorubicin, vincristine, etoposide
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
Publisher:Bentham Science
ISSN:1573-4064
Deposited On:18 Aug 2009 10:02

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