GAR transformylase inhibitor

Details GAR transformylase inhibitor GAR transformylase inhibitor

1988-11-10

1991-03-12

Rollins, John W.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

536 23, C07H 906, A61K 3170, A61K 31395

Patent

active

049994247

ABSTRACT:
The present invention is directed to several multisubstrate adduct inhibitors of glycinamide ribonucleotide transformylase (GAR TFase; E.C. 2.1.2.2), a folate-requiring enzyme of de novo purine biosynthesis. The compounds of the present invention will be useful to provide anti-gout and/or anti-neoplastic therapeutic agents or will serve as potentiators for other such agents. The most prefeffed, potent tight-binding multisubstrate adduct inhibitor of glycinamide ribonucleotide transformylase, is N.sup.10 -[5'-phosphoribosyl-1'-.beta.-aminocarbonylmethyl-1-thioacetyl]-5,8-dideaz afolate, which has the chemical formula: ##STR1##

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Beardsley et al., "Chemistry and Biology of Pteridines, Proc. 8th International Symposium, " B. A. Cooper and Whitehead, V. M., eds. (deGruyter: Berlin, pp. 953-957, 1986).
Temple et al. (1988) vol. 31, pp. 697-700.
Daubner et al. Biochemistry vol. 25, pp. 2951-2957, 1986.

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