Synthesis and anti-integrase evaluation of novel calix[4]arene derivatives containing the triazolyl 1,3-diketo moiety

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• 作者：Zai-Gang Luo^a ; ^{luozi139@163.com" class="auth_mail} ; Yu Zhao^a ; Chao Ma^a ; Xue-Mei Xu^a ; ^{littlekitty@126.com" class="auth_mail} ; Xiao-Mei Zhang^a ; Nian-Yu Huang^b ; Hong-Qiu He^c
• 关键词：HIV-1 integrase inhibitor ; Calix[4]arene derivative ; 1 ; 2 ; 3-Triazole ; 1 ; 3-Diketo ; Strand transfer
• 刊名：Chinese Chemical Letters
• 出版年：May 2014
• 年：2014
• 卷：25
• 期：5
• 页码：737-740
• 全文大小：374 K

文摘

A series of novel calix[4]arene derivatives incorporating two triazolyl 1,3-diketo subunits in alternate positions at the lower rim were synthesized and screened for HIV integrase inhibition activity. The chemical structures of these compounds were confirmed by means of ¹H NMR, ¹³C NMR, and ESI-MS. Preliminary bioassays indicated that calix[4]arene derivatives proved to be more active than p-tert-butylcalix[4]arene derivatives. In particular, compound 4g presented the most potent integrase strand transfer inhibitory activity with an IC₅₀ value of 6.1 渭mol/L.