抗艾滋病药物。33. 单甲基取代的3',4'-二-O-（-）-樟脑酰基-（+）-顺式凯拉内酯（DCK）类似物的合成及抗HIV活性
Anti-AIDS agents. 33. Synthesis and anti-HIV activity of mono-methyl substituted 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) analogues.
作者信息
Xie L, Takeuchi Y, Cosentino L M, Lee K H
机构信息
Natural Products Laboratory, School of Pharmacy, University of North Carolina, Chapel Hill 27599, USA.
出版信息
Bioorg Med Chem Lett. 1998 Aug 18;8(16):2151-6. doi: 10.1016/s0960-894x(98)00367-9.
Four isomeric methyl substituted DCK analogues (2-5) were asymmetrically synthesized from different starting materials. 3-Methyl, 4-methyl, and 5-methyl-3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (2-4) all were extremely potent against HIV-1 replication in H9 lymphocyte cells with EC50 and therapeutic index values of < 4.23 x 10(-7) microM and > 3.72 x 10(8), respectively, which are much better than those of DCK and AZT in this assay.
从不同的起始原料不对称合成了四种甲基取代的DCK异构体类似物（2-5）。3-甲基、4-甲基和5-甲基-3'，4'-二-O-（-）-樟脑酰基-（+）-顺式凯拉内酯（2-4）在H9淋巴细胞中对HIV-1复制均具有极强的抑制作用，其半数有效浓度（EC50）和治疗指数分别小于4.23×10^（-7）微摩尔和大于3.72×10^8，在该实验中比DCK和齐多夫定（AZT）的效果要好得多。
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