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Irreversible enzyme inhibitors. 202. Candidate active-site-directed irreversible inhibitors of 5-fluoro-2'-deoxyuridine phosphorylase from Walker 256 rat tumor derived from 1-benzyl-5-(3-ethoxybenzyl)uracil.

作者信息

Kelley J L, Baker B R

出版信息

J Med Chem. 1982 May;25(5):600-3. doi: 10.1021/jm00347a022.

DOI:10.1021/jm00347a022
PMID:6211547
Abstract

Six candidate irreversible inhibitors of uridine--deoxyuridine phosphorylase (EC 2.4.2.3) from Walker 256 rat tumor were synthesized. These compounds connect a terminal sulfonyl fluoride group to the 1-benzyl moiety of 1-benzyl-5-(3-ethoxybenzyl)uracil (9). Although none of the compounds were irreversible inhibitors, the four 3-[(fluorosulfonyl)benzamido] analogues (14-17) of 9 were good reversible inhibitors of the enzyme which were complexed from 125- to 360-fold better than the substrate, 5-fluoro-2'-deoxyuridine.

摘要

相似文献

1
Irreversible enzyme inhibitors. 202. Candidate active-site-directed irreversible inhibitors of 5-fluoro-2'-deoxyuridine phosphorylase from Walker 256 rat tumor derived from 1-benzyl-5-(3-ethoxybenzyl)uracil.
J Med Chem. 1982 May;25(5):600-3. doi: 10.1021/jm00347a022.
2
5-benzylacyclouridine and 5-benzyloxybenzylacyclouridine, potent inhibitors of uridine phosphorylase.5-苄基阿糖胞苷和5-苄氧基苄基阿糖胞苷，尿苷磷酸化酶的强效抑制剂。
Biochem Pharmacol. 1982 May 15;31(10):1857-61. doi: 10.1016/0006-2952(82)90488-9.
3
Irreversible enzyme inhibitors. CLXXI. Inhibition of FUDR phosphorylase from Walker 256 rat tumor by 5-substituted uracils.不可逆酶抑制剂。第CLXXI篇。5-取代尿嘧啶对Walker 256大鼠肿瘤中氟尿苷磷酸化酶的抑制作用。
J Med Chem. 1970 May;13(3):461-7. doi: 10.1021/jm00297a029.
4
Irreversible enzyme inhibitors. CLXX. Inhibition of FUDR phosphorylase from Walker 256 rat tumor by 1-substituted uracils.不可逆酶抑制剂。CLXX。1-取代尿嘧啶对Walker 256大鼠肿瘤中氟尿苷磷酸化酶的抑制作用。
J Med Chem. 1970 May;13(3):458-61. doi: 10.1021/jm00297a028.
5
Irreversible enzyme inhibitors. CLXIX. Inhibition of FUDR phosphorylase from Walker 256 rat tumor by 6-substituted uracils.不可逆酶抑制剂。CLXIX。6-取代尿嘧啶对Walker 256大鼠肿瘤中氟尿苷磷酸化酶的抑制作用。
J Med Chem. 1970 May;13(3):456-8. doi: 10.1021/jm00297a027.
6
Inhibitor properties of some 5-substituted uracil acyclonucleosides, and 2,2'-anhydrouridines versus uridine phosphorylase from E. coli and mammalian sources.
Biochem Pharmacol. 1987 Dec 1;36(23):4125-8. doi: 10.1016/0006-2952(87)90570-3.
7
Biological activity of two novel inhibitors of uridine phosphorylase.两种新型尿苷磷酸化酶抑制剂的生物活性
Biochem Pharmacol. 1985 Apr 1;34(7):1121-4. doi: 10.1016/0006-2952(85)90621-5.
8
Synthesis of 1-[[2-hydroxy-1-(hydroxymethyl)ethoxy] methyl]-5-benzyluracil and its amino analogue, new potent uridine phosphorylase inhibitors with high water solubility.
J Med Chem. 1985 Jul;28(7):971-3. doi: 10.1021/jm00145a023.
9
Acyclonucleoside analogues consisting of 5- and 5,6-substituted uracils and different acyclic chains: inhibitory properties vs purified E. coli uridine phosphorylase.由5-和5,6-取代的尿嘧啶以及不同的无环链组成的无环核苷类似物：对纯化的大肠杆菌尿苷磷酸化酶的抑制特性
Z Naturforsch C J Biosci. 1987 Mar;42(3):288-96.
10
Ribose-transfer activity from uridine to 5-fluorouracil in Ehrlich ascites tumor cells.艾氏腹水癌细胞中从尿苷到5-氟尿嘧啶的核糖转移活性。
Jpn J Cancer Res. 1990 Jun-Jul;81(6-7):692-700. doi: 10.1111/j.1349-7006.1990.tb02629.x.

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