8,10-dideazatetrahydrofolic acid derivatives

Details 8,10-dideazatetrahydrofolic acid derivatives 8,10-dideazatetrahydrofolic acid derivatives

1990-07-27

1992-12-01

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Implant or insert

424408, 424456, 424464, 424DIG15, 514258, 514937, 514944, 514960, 514962, 514966, 544260, 544279, A61K 902, A61K 964, A61K 31495, C07D47104

Patent

active

051679639

ABSTRACT:
8,10-Dideazatetrahydrofolic acid derivatives of the formula: ##STR1## where R.sub.1 and R.sub.2 are selected from hydrogen and alkyl having from one to about eight carbon atoms and the carboxylates and acid addition salts thereof, showing strong inhibition of L1210 murine leukemia cells in culture, modest inhibition of glycinamide ribotide transformylase and aminoimidazole carboxamide ribotide transferase, and insignificant inhibition of dihydrofolate reductase and thymidylate synthase enzymes.

REFERENCES:
patent: 4684653 (1987-08-01), Taylor et al.
"Synthesis and Biological Activity of L-5-Deazafolic Acid and L-5-Deazaaminopterin: Synthetic Strategies to 5-Deazapteridine's"; Taylor et al., Journal of Organic Chemistry, pp. 4852-4860, 1983.

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