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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Anti-AIDS agents. Part 47:(dagger) synthesis and anti-HIV activity of 3-substituted 3',4'-Di-O-(S)-camphanoyl-(3'R,4'R)-(+)-cis-khellactone derivatives.
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Anti-AIDS agents. Part 47:(dagger) synthesis and anti-HIV activity of 3-substituted 3',4'-Di-O-(S)-camphanoyl-(3'R,4'R)-(+)-cis-khellactone derivatives.

机译:抗艾滋病剂。第47部分:3-取代的3',4'-Di-O-(S)-樟脑酰基-(3'R,4'R)-(+)-顺式-甲壳素衍生物的(匕首)合成和抗HIV活性。

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摘要

Six 3-substituted 3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone derivatives (3-8) were synthesized from 3-methyl DCK (2). 3-Hydroxymethyl DCK (6) exhibited potent anti-HIV activity in H9 lymphocytes with EC(50) and TI values of 1.87x10(-4) &mgr;M and 1.89x10(5), respectively. These values are similar to those of DCK and better than those of AZT in the same assay.
机译:从3-甲基DCK(2)合成了六个3'取代的3',4'-di-O-(S)-樟脑酰基-(+)-顺式-甲壳酮衍生物(3-8)。 3-羟甲基DCK(6)在H9淋巴细胞中表现出有效的抗HIV活性,其EC(50)和TI值分别为1.87x10(-4)M和1.89x10(5)。这些值与DCK的值相似,并且在同一试验中优于AZT的值。

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