Anti-AIDS agents.: Part 56:: Synthesis and anti-HIV activity of 7-thia-di-O-(-)-camphanoyl-(+)-cis-khellactone (7-thia-DCK) analogs
Anti-AIDS agents.: Part 56:: Synthesis and anti-HIV activity of 7-thia-di-O-(-)-camphanoyl-(+)-cis-khellactone (7-thia-DCK) analogs
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DOI：
10.1016/j.bmc.2004.09.038
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发表时间：
2004-12-15
影响因子：
3.5
通讯作者：
Lee, KH
中科院分区：
文献类型：
--
作者：
Chen, Y;Zhang, Q;Lee, KH
合成了两个THIA-DCK类似物(3a，b)，并评价了它们对H9淋巴细胞中HIV-1复制的抑制作用。化合物3a具有较强的抗HIV活性，其EC50值为0.14um，治疗指数为1110。然而，相应的6-叔丁基取代化合物(3b)没有表现出抑制作用。生物活性测试结果表明，THIA-DCK类似物作为潜在的HIV-1抑制剂值得关注。(C)2004爱思唯尔有限公司。保留所有权利。
Two thia-DCK analogs (3a,b) were synthesized and evaluated for inhibition of HIV-1 replication in H9 lymphocytes. Compound 3a showed potent anti-HIV activity with an EC50 value of 0.14 muM and a therapeutic index of 1110. However, the corresponding 6-tert-butyl-substituted compound (3b) showed no suppression. The bioassay results indicated that thia-DCK analogs merit attention as potential HIV-1 inhibitors. (C) 2004 Elsevier Ltd. All rights reserved.