抗艾滋病药物。31. 4-取代的3',4'-二-O-（-）-樟脑酰基-（+）-顺式凯拉内酯（DCK）硫内酯类似物的合成及抗HIV活性
Anti-AIDS agents. 31. Synthesis and anti-HIV activity of 4-substituted 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) thiolactone analogs.
作者信息
Yang Z Y, Xia Y, Xia P, 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 Jun 16;8(12):1483-6. doi: 10.1016/s0960-894x(98)00254-6.
Four DCK-thiolactone analogs (3-6) were synthesized asymmetrically and evaluated for anti-HIV activity against HIV-1 replication in H9 lymphocyte cells. Based on the functionality on the thiolactonecoumarin nucleus, activity was in the order: methyl > H > propyl > benzyl. 4-Methyl-3',4'-di-O-(-)-camphanoyl-(+)-cis-khelthiolactone (4) exhibited extremely potent anti-HIV activity with EC50 and therapeutic index values of 0.00718 microM and > 21,300, respectively.
非对称合成了四种DCK-硫内酯类似物（3-6），并评估了它们对H9淋巴细胞中HIV-1复制的抗HIV活性。基于硫内酯香豆素核上的官能团，活性顺序为：甲基＞氢＞丙基＞苄基。4-甲基-3'，4'-二-O-（-）-樟脑酰基-（+）-顺式-Khel硫内酯（4）表现出极强的抗HIV活性，其EC50和治疗指数值分别为0.00718 microM和＞21300。
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