SYNTHESIS AND BIOLOGIC ACTIVITY OF PURINE 2'-DEOXY-2'-FLUORO-RIBONUCLEOSIDES

被引：18

作者：

THOMAS, HJ

TIWARI, KN

CLAYTON, SJ

SECRIST, JA

MONTGOMERY, JA

机构：

[1] Southern Research Institute, Birmingham, Alabama, P. O. Box 55305

来源：

NUCLEOSIDES & NUCLEOTIDES | 1994年 / 13卷 / 1-3期

基金：

美国国家卫生研究院;

关键词：

D O I：

10.1080/15257779408013243

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The synthesis of 3,5-di-O-benzoyl-2-deoxy-2-fluoro-D-ribofuranosyl bromide (8) and its reaction with 2,6-dichloropurine by fusion and with mercuric cyanide catalysis is described. The resulting 2,6-dichloro-9-(3,5-di-O-benzoyl-2-deoxy-2-fluoro-beta-D-ribofuranosyl)purine (13) was converted to the 2-fluoroadenine (16), the 2-chloroadenine (17), 2,6-diaminopurine (12), and guanine (14) nucleosides by standard procedures. These nucleosides were cytotoxic to a number of cell lines in culture. The 2-haloadenine nucleosides 16 and 17 gave modest increases in lifespan when tested against the P388 leukemia in mice.

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页码：309 / 323

页数：15

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