Enantiomers of gamma methylene 10-deaza aminopterin and process

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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544260, C07D47508

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active

055501281

ABSTRACT:
The biologically active enantiomer of .gamma.-methylene-10-deazaaminopterin (L-MDAM) possessing the L configuration at the .gamma.-methyleneglutamate moiety, which is identical to the absolute configuration at the .alpha.-position of the .gamma.-methyleneglutamic acid isolated from peanut seedlings is provided as well as procedures for its preparation. The compound does not undergo polyglutamylation, is twice as effective as an inhibitor of recombinant human dihydrofolate reductase, and exhibits outstanding growth inhibitory activity in a large variety of human tumor cells in culture. The biochemical and pharmacological results established the utility of L-MDAM as a therapeutic agent for the treatment of human neoplastic diseases.

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