2-(3-arylacryloyl)-3-Methylquinoxaline 1,4-Dioxides as Potential Hypoxic Selective Cytotoxins

Document Type

Article

Publication Date

2008

Publication Source

HeterocyclicCommunications

Volume Number

14

Issue Number

5

First Page

385

Last Page

388

Publisher

Freund Publishing House Ltd.

ISSN

0793-0283

Abstract

The synthesis of a series of 2-(3-arylacryloyl)-3-methylquinoxaline 1,4-dioxides is reported. In-vitro cytotoxic activity of these compounds was evaluated via the MTT assay in B16 murine melanoma and L1210 murine leukemia cell lines. A dichloro analogue was found to be the most cytotoxic and was > 30-fold more active than the quinoxaline control (IC50 = 2 vs. 67 mu M in L1210, respectively). These results suggest that compounds containing two bioactive moieties could be developed as hypoxic selective cytotoxins.

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