Citation: Zai-Gang Luo, Yu Zhao, Chao Ma, Xue-Mei Xu, Xiao-Mei Zhang, Nian-Yu Huang, Hong-Qiu He. Synthesis and anti-integrase evaluation of novel calix[4]arene derivatives containing the triazolyl 1, 3-diketo moiety[J]. Chinese Chemical Letters, ;2014, 25(05): 737-740. doi: 10.1016/j.cclet.2014.03.012 shu

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

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a College of Chemical Engineering, Anhui University of Science & Technology, Huainan 232001, China;
2.
b College of Chemistry and Life Sciences, China Three Gorges University, Yichang 443002, China;
3.
c Chongqing Center for Biomedicines and Medical Equipment, Chongqing Academy of Science and Technology, Chongqing 401123, China

Corresponding author: Zai-Gang Luo, Xue-Mei Xu,
Received Date: 13 December 2013
Available Online: 20 February 2014
Fund Project: The authors gratefully thank the National Natural Science Foundation of China (Nos.21102003, 21102084, 81202438) (Nos.21102003, 21102084, 81202438)

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.
- HIV-1 integrase inhibitor,
- Calix[4]arene derivative,
- 1,2,3-Triazole,
- 1,3-Diketo,
- Strand transfer
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沈阳化工大学材料科学与工程学院沈阳 110142