Anti-AIDS agents. Part 56: Synthesis and anti-HIV activity of 7-thia-di-O-(−)-camphanoyl-(+)-cis-khellactone (7-thia-DCK) analogs

…, N Kilgore, C Wild, SL Morris-Natschke, KH Lee

文献索引：Chen, Ying; Zhang, Qian; Zhang, Beina; Xia, Peng; Xia, Yi; Yang, Zheng-Yu; Kilgore, Nicole; Wild, Carl; Morris-Natschke, Susan L.; Lee, Kuo-Hsiung Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 24 p. 6383 - 6387

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被引用次数: 43

摘要

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 μM 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.