Synthesis and anti-integrase evaluation of novel calix[4]arene derivatives containing the triazolyl 1,3-diketo moiety |
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| Authors: | Zai-Gang Luo, Yu Zhao, Chao Ma, Xue-Mei Xu, Xiao-Mei Zhang, Nian-Yu Huang, Hong-Qiu He |
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| Affiliation: | a College of Chemical Engineering, Anhui University of Science & Technology, Huainan 232001, China;b College of Chemistry and Life Sciences, China Three Gorges University, Yichang 443002, China;c Chongqing Center for Biomedicines and Medical Equipment, Chongqing Academy of Science and Technology, Chongqing 401123, China |
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| Abstract: | 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 μmol/L. |
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| Keywords: | HIV-1 integrase inhibitor Calix arene derivative 1 2 3-Triazole 1 3-Diketo Strand transfer |
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