Synthesis and Biological Activities of Sugar-Modified 2-(p-n-Butylanilino)-2′-deoxyadenosine Analogues |
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Authors: | Toyofumi Yamaguchi Kunie Sato Mineo Saneyoshi |
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Institution: | Department of Biological Sciences , The Nishi-Tokyo University , 2525, Yatsuzawa, Uenohara-machi, Kitatsuru-gun, Yamanashi, 409-01, Japan |
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Abstract: | Abstract Several sugar-modified 2-(p-n-butylanilino)-2′-deoxyadenosine analogues, including arabino and 2′(R)-azido-2′-deoxy analogues and their 5′-triphosphates were synthesized. These nucleosides thus obtained exhibited moderate cytotoxicity against P-388 leukemic cells in culture (IC50 = 13–24 μ). In contrast to above results, the 5′-triphosphates have been shown to exert strong and selective inhibitory effects on mammalian DNA polymerase α (Ki= 0.02–0.04 μ). |
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