Synthetic Nucleosides and Nucleotides. XXVII. Selective Inhibition of Deoxyribonucleic Acid Polymerase α by 1-β-D-Arabinofuranosyl-5-styryluracil 5'-Triphosphates and Related Nucleotides : Influence of Hydrophobic and Steric Factors on the Inhibitory Acti
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概要
- 論文の詳細を見る
Eight kinds of 5-substituted 1-β-D-arabinofuranosyluracil 5'-triphosphates ((E)-(3-nitrostyryl)(6), (E)-(3-aminostyryl)(9), (E)-(4-nitrostyryl)(7), (E)-(4-aniinostyryl)(10), (E)-styryl(8), phenethyl(11), (RS)-(3-azido-2-hydroxypropyl)(17), and (RS)-(3-amino-2-hydroxypropyl)(18) derivatives) were synthesized. Among these analogs, araUTPs bearing strongly hydrophobic styryl groups at the 5-position (6-10) were shown to have selective and strong inhibitory, action on deoxyribonucleic acid (DNA) polymerase α purified from cherry salmon (Oncorhynclrus mnasou) testes. The 5-azidopropyl derivative(17) also inhibited this polymerase. The compounds with a nitro and an amino group on the 5-styryl substituent showed essentially the same activity, but the 5-phenethyl derivative(11) and the 5-aminopropyl derivative(18) showed greatly reduced inhibitory action. On the other hand, in the case of DNA polymerase β, all the analogs showed similar inhibitory effects. The influence of hydrophobic and steric effects of substituents at the 5-position of araUTP on DNA polymerases a and β are discussed.
- 公益社団法人日本薬学会の論文
- 1987-12-25
著者
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伊豆田 俊二
Research Institute For Disease Mechanism And Control Nagoya University School Of Medicine
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Izuta Shunji
Research Institute For Disease Mechanism And Control Nagoya University School Of Medicine
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実吉 峯郎
Faculty of Pharmaceutical Sciences, Hokkaido University
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実吉 峯郎
Faculty Of Pharmaceutical Sciences Hokkaido University
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伊豆田 俊二
Faculty of Pharmaceutical Sciences, Hokkaido University
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