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Makoto Koizumi Rika Koga Hitoshi Hotoda Kenji Momota Toshinori Ohmine Hidehiko Furukawa Toshinori Agatsuma Takashi Nishigaki Koji Abe Toshiyuki Kosaka Shinya Tsutsumi Junko Sone Masakatsu Kaneko Satoshi Kimura Kaoru Shimada 《Bioorganic & medicinal chemistry》1997,5(12):2235-2243
We have determined that hexadeoxyribonucleotides (5′TGGGAG3′), with modified aromatic groups such as a trityl group at the 5′-end, have anti-HIV-1 activity in vitro. The 6-mer bearing a 3,4-dibenzyloxybenzyl (3,4-DBB) group at the 5′-end had the most potent activity and the least cytotoxicity. When the 3′-end of the 5′-(3,4-DBB)-modified 6-mer was substituted with a 2-hydroxyethylphosphate, a 2-hydroxyethylthiophosphate, or a methylphosphate group at the 3′-end, anti-HIV-1 activity increased. Moreover, among various 3′- and 5′-end-modified 6-mers that were tested, the 6-mer (R-95288) bearing a 3,4-DBB group at the 5′-end and a 2-hydroxyethylphosphate group at the 3′-end was the most stable, when incubated with mouse, rat, or human plasma. Therefore, R-95288 was chosen as the best candidate for possible use in therapy on the basis of its anti-HIV-1 activity. 相似文献
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