Design, synthesis, and evaluation of potential GAR and AICAR transformylase inhibitors

…, J Ramcharan, LT Gooljarsingh, SJ Benkovic

文献索引：Boger, Dale L.; Kochanny, Monica J.; Cai, Hui; Wyatt, Diane; Kitos, Paul A.; Warren; Ramcharan; Gooljarsingh, Lata T.; Benkovic, Stephen J. Bioorganic and Medicinal Chemistry, 1998 , vol. 6, # 6 p. 643 - 659

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被引用次数: 18

摘要

In preceding studies,[1]we detailed the preparation and evaluation of potent inhibitors of glycinamide ribonucleotide transformylase (GAR Tfase) and aminoimidazole carboxamide ribonucleotide transformylase (AICAR Tfase), folate dependent enzymes responsible for the transfer of a formyl group to GAR and AICAR in the de novo synthesis of purines, based on the 5,8,10-trideazafolate core. The most effective of the agents incorporated a reactive, electrophilic group ...