Anti-AIDS agents. Part 62: Anti-HIV activity of 2′-substituted 4-methyl-3′, 4′-di-O-(−)-camphanoyl-(+)-cis-khellactone (4-methyl DCK) analogs

…, ZY Yang, D Yu, SL Morris-Natschke, KH Lee

Index: Zhang, Qian; Chen, Ying; Xia, Peng; Xia, Yi; Yang, Zheng-Yu; Yu, Donglei; Morris-Natschke, Susan L.; Lee, Kuo-Hsiung Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 23 p. 5855 - 5857

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Citation Number: 18

Abstract

Four 4-methyl-3′, 4′-di-O-(−)-camphanoyl-(+)-cis-khellactone (4-methyl DCK) analogs (7a– d) with different alkyl substituents at the 2′-position were synthesized and evaluated for inhibition of HIV-1 replication in H9 lymphocytes. 2′-Methyl-2′-ethyl-4-methyl DCK (7b) was more potent (EC50= 0.22 μM, TI> 175) than the other three compounds (7a, 7c, and 7d), but significantly less potent than 4-methyl DCK (2, EC50= 0.0059 μM, TI> 6600). The ...