The Use of Benzoin as a Privileged Structure: Synthesis, Characterization, Crystalline Form and an In Vitro Biological Evaluation of 1,2-Diphenyl-2-[1,2,3]triazol-1-yl-ethanol Derivatives

苯偶姻作为一种优势结构的应用:1,2-二苯基-2-[1,2,3]三唑-1-基乙醇衍生物的合成、表征、晶体形式及体外生物学评价

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Abstract

A collection of 40 derivatives of 1,2-diphenyl-2-[1,2,3]triazol-1-yl-ethanol was obtained through a sequence of reactions, starting with benzoin as the initial raw material and using the CuAAC reaction as the key step in this process. The structure of a pair of these compounds was ultimately corroborated by single-crystal X-ray diffraction studies, which also reveals important O-H···N interactions. The antimicrobial activity of synthesized 1,2,3-triazoles was assessed against strains that include Candida albicans and Staphylococcus aureus. The antiproliferative properties of some of these novel compounds were also tested using a variety of tumor cell lines, including U251 (human glioblastoma), PC-3 (human prostate cancer cell line), K562 (human leukemia), HCT-15 (human colorectal adenocarcinoma), MCF-7 (human breast adenocarcinoma), and SKLU (human lung adenocarcinoma).

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