期刊
MOLECULES
卷 25, 期 4, 页码 -出版社
MDPI
DOI: 10.3390/molecules25040986
关键词
longifolene-derived tetralone; 1,2,4-triazole; antiproliferative activity; synthesis
资金
- National Key R&D Program of China [2018YFD0600401]
- National Natural Science Foundation of China [31870556]
Seventeen novel 2-(5-amino-1-(substituted sulfonyl)-1H-1,2,4-triazol-3-ylthio)-6-isopropyl-4,4-dimethyl-3,4-dihydronaphthalen-1(2H)-one compounds were synthesized from the abundant and naturally renewable longifolene and their structures were confirmed by FT-IR, NMR, and ESI-MS. The in vitro cytotoxicity of the synthesized compounds was evaluated by standard MTT assay against five human cancer cell lines, i.e., T-24, MCF-7, HepG2, A549, and HT-29. As a result, compounds 6d, 6g, and 6h exhibited better and more broad-spectrum anticancer activity against almost all the tested cancer cell lines than that of the positive control, 5-FU. Some intriguing structure-activity relationships were found and are discussed herein by theoretical calculation.
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