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

Autor:	Chao Ma, Nian-Yu Huang, Hong-Qiu He, Zaigang Luo, Xiao-Mei Zhang, Yu Zhao, Xuemei Xu
Rok vydání:	2014
Předmět:	chemistry.chemical_compound 1 2 3-Triazole biology Stereochemistry Chemistry biology.protein Proton NMR Moiety General Chemistry Carbon-13 NMR IC50 Integrase Strand transfer
Zdroj:	Chinese Chemical Letters. 25:737-740
ISSN:	1001-8417
DOI:	10.1016/j.cclet.2014.03.012
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::0014f47e63441b5337cc581fc75bb94f https://doi.org/10.1016/j.cclet.2014.03.012 Zobrazit plný text záznamu Full Text from ScienceDirect