SYNTHESIS AND BIOLOGICAL EFFECTS OF N-(2-PHOSPHONOMETHOXYETHYL) DERIVATIVES OF DEAZAPURINE BASES

被引:21
作者
DVORAKOVA, H
HOLY, A
机构
关键词
D O I
10.1135/cccc19931419
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Analogs of antiviral 9-(2-phosphonomethoxyethyl)adenine (PMEA, II), containing modified purine bases 1-deazaadenine (VII), 3-deazapurine (XI), 7-deaza-7-cyanoadenine (XIIIb) and 3-deazaguanine (XXIb), were prepared by alkylation of the heterocyclic bases with bis(2-propyl) 2-chloroethoxymethylphosphonate (V) in dimethylformamide in the presence of sodium hydride or cesium carbonate. The obtained protected derivatives were deblocked with bromotrimethylsilane to give the phosphonic acids. 3-DeazaPMEG (XXIb) is active against DNA viruses and exhibits a marked cytostatic effect against L-1210 leukemia.
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页码:1419 / 1429
页数:11
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