Novel Triazole–Diquinothiazine Hybrids Modulating Apoptosis and Stress Pathways in Colorectal Cancer Cells

Background/Objectives: Colorectal cancer is one of the most common malignancies worldwide and is frequently associated with dysregulation of apoptosis, oxidative stress, and the p53 regulatory axis. The development of novel compounds capable of modulating these pathways remains an important challenge in anticancer drug discovery. This study aimed to evaluate the biological activity of newly synthesized triazole–diquinothiazine derivatives in colorectal cancer cells and to identify the most promising lead compound for further development. Methods: The synthesized derivatives were evaluated in HCT116 colorectal cancer cells harboring wild-type TP53 and in normal BEAS-2B cells. Cytotoxicity, apoptosis, cell cycle distribution, intracellular reactive oxygen species (ROS) generation, and the expression of genes associated with apoptosis, oxidative stress, and inflammatory response were analyzed. Results: The investigated compounds exhibited diverse biological effects, including modulation of apoptosis, cell cycle progression, and oxidative stress. Among the tested derivatives, compound B5 demonstrated the most favorable biological profile, characterized by a more pronounced biological response in HCT116 cells than in BEAS-2B cells, increased ROS generation, reduced MDM2 expression, and a marked induction of early apoptosis. Conclusions: The obtained results indicate that triazole–diquinothiazine derivatives represent promising lead structures for further optimization. In particular, compound B5 warrants additional mechanistic and preclinical studies to evaluate its potential as a candidate for colorectal cancer therapy.

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Publication Details

Journal
Pharmaceuticals
Published
2026-07-23
DOI
https://doi.org/10.3390/ph19081133
Primary Topic
Phenothiazines and Benzothiazines Synthesis and Activities
Type
article
Field-Weighted Citation Impact
0.00

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article

Novel Triazole–Diquinothiazine Hybrids Modulating Apoptosis and Stress Pathways in Colorectal Cancer Cells

Magdalena Skonieczna, Małgorzata Jeleń, Beata Morak‐Młodawska, Klaudia Giercuszkiewicz-Haśnik
Pharmaceuticals
Phenothiazines and Benzothiazines Synthesis and Activities
article

Novel Triazole–Diquinothiazine Hybrids Modulating Apoptosis and Stress Pathways in Colorectal Cancer Cells

Magdalena Skonieczna, Małgorzata Jeleń, Beata Morak‐Młodawska, Klaudia Giercuszkiewicz-Haśnik
article en

Abstract

Background/Objectives: Colorectal cancer is one of the most common malignancies worldwide and is frequently associated with dysregulation of apoptosis, oxidative stress, and the p53 regulatory axis. The development of novel compounds capable of modulating these pathways remains an important challenge in anticancer drug discovery. This study aimed to evaluate the biological activity of newly synthesized triazole–diquinothiazine derivatives in colorectal cancer cells and to identify the most promising lead compound for further development. Methods: The synthesized derivatives were evaluated in HCT116 colorectal cancer cells harboring wild-type TP53 and in normal BEAS-2B cells. Cytotoxicity, apoptosis, cell cycle distribution, intracellular reactive oxygen species (ROS) generation, and the expression of genes associated with apoptosis, oxidative stress, and inflammatory response were analyzed. Results: The investigated compounds exhibited diverse biological effects, including modulation of apoptosis, cell cycle progression, and oxidative stress. Among the tested derivatives, compound B5 demonstrated the most favorable biological profile, characterized by a more pronounced biological response in HCT116 cells than in BEAS-2B cells, increased ROS generation, reduced MDM2 expression, and a marked induction of early apoptosis. Conclusions: The obtained results indicate that triazole–diquinothiazine derivatives represent promising lead structures for further optimization. In particular, compound B5 warrants additional mechanistic and preclinical studies to evaluate its potential as a candidate for colorectal cancer therapy.

PharmaceuticalsVol. 19(8)
Silesian University of Technology (PL), Medical University of Silesia (PL), University of Silesia in Katowice (PL)
Silesian University of Technology
Good health and well-being
Openalex Percentile: Top 15%
Phenothiazines and Benzothiazines Synthesis and Activities
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