Bioorganic and Medicinal Chemistry p. 1817 - 1830 (1997)
Update date:2022-07-31
Topics:
Boger, Dale L.
Haynes, Nancy-Ellen
Kitos, Paul A.
Warren, Mark S.
Ramcharan, Joseph
Marolewski, Ariane E.
Benkovic, Stephen J.
The synthesis of 10-formyl-5,8,10-trideazafolic acid (3) as a potential inhibitor of glycinamide ribonucleotide transformylase (GAR Tfase) is reported. The target compound was prepared by a convergent synthesis utilizing the alkylation of hydrazone 5 with benzylic bromide 6 to construct the core heterocycle 7. The aldehyde 3 and related agents were evaluated as inhibitors of purN GAR Tfase and avian AICAR Tfase. Compound 3 exhibited potent inhibition of GAR Tfase with a K(i) of 0.26 ± 0.05 μM. In contrast, 3 exhibited more moderate inhibition of aminoimidazole carboxamide ribonucleotide transformylase (AICAR Tfase), with K(i) of 7.6 ± 1.5 μM.
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Doi:10.1021/om9707228
(1997)Doi:10.1016/S0040-4039(97)10147-2
(1997)Doi:10.1248/cpb.45.1734
(1997)Doi:10.1016/j.bmcl.2017.12.056
(2018)Doi:10.1021/ja01009a027
(1968)Doi:10.1055/s-1997-1017
(1997)
