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DL-threo-beta-Fluoroaspartate and DL-threo-beta-fluoroasparagine: selective cytotoxic agents for mammalian cells in culture.

Abstract：

:Absolute configuration assignments have been made for the diastereomers of DL-beta-fluoroaspartate by X-ray analysis. The cytotoxicity of these isomers against various mammalian cells was examined. DL-threo-beta-Fluoroaspartate shows selective cytotoxicity. Growth of the most sensitive cells is completely inhibited by 13 micrometers DL-threo-beta-fluoroaspartate in the presence of 100 micrometers L-aspartate, a component of the culture medium. A difference in the rate of transport of DL-beta-fluoroaspartate among the cells studied is an important factor determining cell specificity. For those cells that are sensitive to DL-beta-fluoroaspartate, the threo isomer is, in all cases, more potent than the erythro isomer. Radioactivity derived from L-threo-beta-fluoro[14C]aspartate is incorporated into proteins at a rate comparable to the rate of incorporation from L-[14C]aspartate. We synthesized DL-threo-beta-fluoroasparagine. This compound is also cytotoxic but less specific and less potent than DL-threo-beta-fluoroaspartate. However, the cell specificity can be enhanced in the presence of 1 mM L-aspartate, which can protect some cells but not others from the cytotoxic effects of DL-threo-beta-fluoroasparagine. Jensen sarcoma cells, which require asparagine, are not protected by L-aspartate. Therefore, a combination of L-aspartate and DL-threo-beta-fluroasparagine can be used to inhibit specifically the growth of asparagine-requiring tumors.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Stern AM,Foxman BM,Tashjian AH Jr,Abeles RH

doi

10.1021/jm00347a013

subject

Has Abstract

pub_date

1982-05-01 00:00:00

pages

544-50

issue

5

eissn

0022-2623

issn

1520-4804

journal_volume

25

pub_type

杂志文章

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