Anti-AIDS agents.: Part 58:: Synthesis and anti-HIV activity of 1-thia-di-O-(-)-camphanoyl-(+)-cis-khellactone (1-thia-DCK) analogues
Anti-AIDS agents.: Part 58:: Synthesis and anti-HIV activity of 1-thia-di-O-(-)-camphanoyl-(+)-cis-khellactone (1-thia-DCK) analogues
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DOI：
10.1016/j.bmcl.2004.03.051
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发表时间：
2004-06-21
影响因子：
2.7
通讯作者：
Lee, KH
中科院分区：
文献类型：
--
作者：
Xia, P;Yin, ZJ;Lee, KH
合成了两种1-thia-DCK类似物（9a和9 b），并评价了其对H9淋巴细胞中HIV-1复制的抑制作用。化合物9a显示出优异的抗HIV活性，其EC 50值为0.00012 μ M，治疗指数为1，408，000。化合物9 b活性较低，EC 50和TI值分别为3.11 μ M和62.3。生物测定结果表明thia-DCK类似物作为潜在的HIV-1抑制剂值得关注。(C)2004 Elsevier Ltd.保留所有权利。
Two 1-thia-DCK analogues (9a and 9b) were synthesized and evaluated for inhibition of HIV-1 replication in H9 lymphocytes. Compound 9a showed excellent anti-HIV activity with an EC50 value of 0.00012 muM and therapeutic index of 1,408,000. Compound 9b was less active with EC50 and TI values of 3.11 muM and 62.3, respectively. The bioassay results indicated that thia-DCK analogues merit attention as potential HIV-1 inhibitors. (C) 2004 Elsevier Ltd. All rights reserved.