# 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

**Authors:** Noé Martínez-Romero, Mario Valle-Sánchez, Marco A. García-Eleno, Carlos A. González-González, David Corona-Becerril, Lizbeth Triana-Cruz, Diego Martínez-Otero, María Teresa Ramírez-Apan, David Morales-Morales, Jorge Andrés Ornelas-Guillén, Erick Cuevas-Yañez

PMC · DOI: 10.3390/molecules31010170 · Molecules · 2026-01-01

## TL;DR

This paper explores the synthesis and biological evaluation of new compounds based on benzoin, showing potential antimicrobial and anticancer properties.

## Contribution

The study introduces a novel synthetic approach using benzoin and CuAAC to create 1,2-diphenyl-2-[1,2,3]triazol-1-yl-ethanol derivatives with antimicrobial and antiproliferative activities.

## Key findings

- The compounds showed antimicrobial activity against Candida albicans and Staphylococcus aureus.
- Some derivatives exhibited antiproliferative effects on various tumor cell lines.
- Single-crystal X-ray diffraction confirmed the structure and revealed O-H···N interactions.

## 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).

## Linked entities

- **Chemicals:** benzoin (PubChem CID 8400)
- **Diseases:** glioblastoma (MONDO:0018177), prostate cancer (MONDO:0005159), leukemia (MONDO:0004355), colorectal adenocarcinoma (MONDO:0005008), breast adenocarcinoma (MONDO:0004988), lung adenocarcinoma (MONDO:0005061)
- **Species:** Homo sapiens (taxon 9606)

## Full-text entities

- **Diseases:** lung adenocarcinoma (MESH:D000077192), leukemia (MESH:D007938), tumor (MESH:D009369), colorectal adenocarcinoma (MESH:D003110), glioblastoma (MESH:D005909), prostate cancer (MESH:D011471), breast adenocarcinoma (MESH:D001943)
- **Chemicals:** 1,2,3-triazoles (-), Benzoin (MESH:D001573)
- **Species:** Candida albicans (species) [taxon 5476], Homo sapiens (human, species) [taxon 9606], Staphylococcus aureus (species) [taxon 1280]

## Full text

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## Figures

8 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12787705/full.md

## References

57 references — full list in the complete paper: https://tomesphere.com/paper/PMC12787705/full.md

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Source: https://tomesphere.com/paper/PMC12787705