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5-氟-2'-脱氧尿苷(FUdR)酯的非酶促水解和酶促水解

Nonenzymatic and enzymatic hydrolysis of 5-fluoro-2'-deoxyuridine (FUdR) esters.

作者信息

Kawaguchi T, Fukushima S, Hayashi Y, Nakano M

机构信息

Faculty of Pharmaceutical Sciences, Josai University, Saitama, Japan.

出版信息

Pharm Res. 1988 Nov;5(11):741-4. doi: 10.1023/a:1015972214747.

DOI:10.1023/a:1015972214747
PMID:2977648
Abstract

The chemical and enzymatic reactivity of 5-fluoro-2'-deoxyuridine prodrugs esterified at the 3' and 5' positions with several acyl groups has been investigated. The enzymatic reactivity was affected by the acyl structure, the site of esterification, and the number of esters in the prodrug molecule.

摘要

对在3'和5'位被几种酰基酯化的5-氟-2'-脱氧尿苷前药的化学和酶促反应活性进行了研究。酶促反应活性受酰基结构、酯化位点以及前药分子中酯的数量影响。

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引用本文的文献

1
Amino acid ester prodrugs of floxuridine: synthesis and effects of structure, stereochemistry, and site of esterification on the rate of hydrolysis.氟尿苷的氨基酸酯前药:合成以及结构、立体化学和酯化位点对水解速率的影响
Pharm Res. 2003 Sep;20(9):1381-8. doi: 10.1023/a:1025745824632.

本文引用的文献

1
A pharmacokinetic analysis program (multi) for microcomputer.一种用于微型计算机的药代动力学分析程序(多功能)。
J Pharmacobiodyn. 1981 Nov;4(11):879-85. doi: 10.1248/bpb1978.4.879.
2
Antitumor activity of 3',5'-diesters of 5-fluoro-2'-deoxyuridine against murine leukemia L1210 cells.
Cancer Chemother Pharmacol. 1981;6(1):19-23. doi: 10.1007/BF00253005.
3
3',5'-Diesters of 5-fluoro-2'-deoxyuridine and thymidine: hydrolysis by esterases in human, mouse, and insect tissue.5-氟-2'-脱氧尿苷和胸苷的3',5'-二酯:在人、小鼠和昆虫组织中被酯酶水解
Biochem Pharmacol. 1966 May;15(5):627-44. doi: 10.1016/0006-2952(66)90030-x.
4
3',5'-diesters of 5-fluoro-2'-deoxyuridine: synthesis and biological activity.
Biochem Pharmacol. 1965 Nov;14(11):1605-19. doi: 10.1016/0006-2952(65)90015-8.
5
Activity of esterase in the hydrolysis of 3',5'-diesters of 5-fluoro-2'-deoxyuridine in relation to the structure of the diester prodrugs.酯酶在5-氟-2'-脱氧尿苷3',5'-二酯水解中的活性与二酯前药结构的关系
Chem Pharm Bull (Tokyo). 1985 Jan;33(1):301-7. doi: 10.1248/cpb.33.301.
6
Selective anticancer effects of 3',5'-dioctanoyl-5-fluoro-2'-deoxyuridine, a lipophilic prodrug of 5-fluoro-2'-deoxyuridine, dissolved in an oily lymphographic agent on hepatic cancer of rabbits bearing VX-2 tumor.
Cancer Res. 1987 Apr 1;47(7):1930-4.
7
Specificity of esterases and structure of prodrug esters. II. Hydrolytic regeneration behavior of 5-fluoro-2'-deoxyuridine (FUdR) from 3',5'-diesters of FUdR with rat tissue homogenates and plasma in relation to their antitumor activity.酯酶的特异性与前药酯的结构。II. 5-氟-2'-脱氧尿苷(FUdR)3',5'-二酯在大鼠组织匀浆和血浆中的水解再生行为及其与抗肿瘤活性的关系
Chem Pharm Bull (Tokyo). 1985 Apr;33(4):1652-9. doi: 10.1248/cpb.33.1652.