Thiophene substituted antitumor antifolates

Details Thiophene substituted antitumor antifolates Thiophene substituted antitumor antifolates

1992-05-13

1993-11-09

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

052602966

ABSTRACT:
A new thiophene substituted antitumor antifolate, N{[5-(2,4-diamino-6-pteridinyl)ethyl]2-theonyl}-L-glutamic acid having the structural formula 1 is provided, as well as methods for its preparation. The new thiophene substituted antifolate 1 is a very potent inhibitor of the enzyme dihydrofolate reductase, undergoes moderate polyglutamylation and is transported to tumor cells more effectively than methotrexate. Compound 1 is an excellent inhibitor of tumor cells growth in culture, the potency being superior to methotrexate against CCRF-CEM human lukemia cells.

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