Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1990-08-03
1991-12-17
Daus, Donald G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
544260, A61K 31505
Patent
active
050735543
ABSTRACT:
Two new non-polyglutamatable glutamic acid derivatives in the antifolate series are provided as well as procedures for their preparation. These compounds are: 4-amino-4-deoxy-10-methylpteroyl-.tau.-methyleneglutamic acid (1) and 4-amino-4-deoxy-10-methylpteroyl-.beta.-hydroxyglutamic acid (2). Compounds 1 and 2 do not undergo polyglutamylation as determined by their inability to serve as substrates for folylpolyglutamate synthetase (FPGS), and they are powerful inhibitors of human dihydrofolate reductase (DHFR). Both compounds 1 and 2 are powerful inhibitors of the growth of Manca human lymphoma, human leukemia (CCRF-CEM) and H35 hepatoma cells.
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