10-(2-benzoxazolcarbonyl)-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid: a potential inhibitor of GAR transformylase and AICAR transformylase.
10-(2-benzoxazolcarbonyl)-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid: a potential inhibitor of GAR transformylase and AICAR transformylase.
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10-(2-苯并恶唑羰基)-5,10-二脱氮杂-无环-5,6,7,8-四氢叶酸：GAR 转化酶和 AICAR 转化酶的潜在抑制剂。
DOI：
10.1016/s0968-0896(03)00457-7
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发表时间：
2003
影响因子：
3.5
通讯作者：
Boger,DaleL
中科院分区：
文献类型：
--
作者：
Marsilje,ThomasH;Hedrick,MichaelP;Desharnais,Joel;Capps,Kevin;Tavassoli,Ali;Zhang,Yan;Wilson,IanA;Benkovic,StephenJ;Boger,DaleL
报道了10-（2-苯并恶唑羰基）- ddacthf(1)作为甘氨酸酰胺核糖核苷酸转化酶（GAR）和氨基咪唑羧化酶（AICAR）抑制剂的设计和合成。酮1和相应的醇13对GAR Tfase和AICAR Tfase的抑制作用进行了评价，发现前者是重组人（rh） GAR Tfase （Ki=600 nM）的有效抑制剂。
The design and synthesis of 10-(2-benzoxazolcarbonyl)-DDACTHF (1) as an inhibitor of glycinamide ribonucleotide transformylase (GAR Tfase) and aminoimidazole carboxamide transformylase (AICAR Tfase) are reported. Ketone 1 and the corresponding alcohol 13 were evaluated for inhibition of GAR Tfase and AICAR Tfase and the former was found to be a potent inhibitor of recombinant human (rh) GAR Tfase (Ki=600 nM).