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Potential anticancer agents: 5-(N-substituted-aminocarbonyl)- and 5-(N-substituted-aminothiocarbonyl)-5,6,7,8-tetrahydrofolic acids.

作者信息

Temple C, Elliott R D, Montgomery J A

机构信息

Kettering-Meyer Laboratory, Southern Research Institute, Birmingham, Alabama 35255-5305.

出版信息

J Med Chem. 1988 Mar;31(3):697-700. doi: 10.1021/jm00398a034.

DOI:10.1021/jm00398a034
PMID:3346883
Abstract

5-[[N-[(Ethoxycarbonyl)alkyl]amino]carbonyl] (6-9) and the corresponding aminothiocarbonyl (12-15) derivatives of 5,6,7,8-tetrahydrofolic acid were prepared as multisubstrate analogues of the substrate--cofactor adduct in the reactions catalyzed by the folate-mediated one-carbon transfer reactions. Evaluation in vitro showed that 7 (alkyl = hexyl) was cytotoxic to H.Ep.-2 cells (ED50, 4 microM) but noncytotoxic to proliferating L1210 cells. No activity was observed for 7 against the P388 leukemia in mice.

摘要

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