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Journal of the Korean Chemical Society (JKCS)

ISSN 1017-2548(Print)
ISSN 2234-8530(Online)
Volume 19, Number 6
JKCSEZ 19(6)
December 20, 1975 

 
Title
Synthesis of 1-(4-Thio-α,β-D-ribofuranosyl)-5-halogenouracils (Ⅱ). 5-Fluoro-4'-thiouridine and 5-Chloro-4'-thio-uridine

5-할로겐 치환된 Uracil의 4-Thiosugar Nucleosides의 합성에 관한 연구 (제2보). 5-Fluoro-4'-thiouridine과 5-Chloro-4'-thiouridine의 합성
Author
Jack C, Kim, Won-Jei Cho, Miroslay Bobek, Roy L. Whistler

김정균, 조원제, 보벡크, 윗슬러
Keywords
Abstract
Unusual pyrimidine nucleoside인 5-fluoro-4'-thiouridine과 5-Chloro-4'-thiouridine을 5-fluoro-와 5-chlorouracil의 2,4-bis(trimethylsilyl) 유도체들을 만든후, 축합반응하여 합성하였다. Leukemia 1210 cell과 Streptococcus faecium에 대한 기초 생물화학적인 예비시험에 의하면 5-fluoro-4'-thiouridine은 5-fluorouridine보다 억제효과가 월등하여 항암제로서의 전망여하는 앞으로의 임상 화학적인 결과로 구명될것 이라고 예상된다.

The syntheses of anomeric mixtures of 1-(4-thio-α,β-D-ribofuranosyl)-5-fluoro-and 5-chlorouracils from their corresponding bis(trimethylsilyl) derivatives of 5-halogenouracils and 2,3,5-tri-O-acetyl-4-thio-α,β-D-ribofuranosyl chloride are described. Preliminary biochemical studies showed that in leukemia 1210 cells and Streptococcus faecium, the β-anomeric 5-chloro-4'-thionucleoside is not greatly different from the corresponding 4'-oxygen analog. However, the 5-fluoro-4'-thionucleoside showed a growth inhibitory effect more than that of the oxygen counterpart. The potential chemotherapeutic use of the analog is to warrant further study.

Page
438 - 442
Full Text
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