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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

[ Vol. 2 , Issue. 2 ]

Author(s):

Roberta Loddo, Paolo La Colla, Bernardetta Busonera, Gabriella Collu, Giuseppe Paglietti, Sandra Piras, Antonio Carta and Mario Loriga   Pages 113 - 122 ( 10 )

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.

Keywords:

etoposide, vincristine, doxorubicin, P-glycoprotein inhibitors, multidrug resistance, antiproliferative activity, quinoxalines, 2-Quinoxalinones

Affiliation:

Dipartimento FarmacoChimico Tossicologico, via Muroni 23/a, 07100 Sassari-Italy.



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