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SarveAhrabi Y, Aqa Abedi S, Ahmadirad M, Zarrabi Ahrabi N. Anticancer 1,3-thiazole Derivatives: In Vitro Evaluation and in Silico Tubulin/Lipoxygenase Inhibition. Pharm Biomed Res 2026; 12 (2) :87-98
URL: http://pbr.mazums.ac.ir/article-1-679-en.html

Background: Addressing cancer treatment and drug resistance is critical because cancer remains a leading cause of death worldwide. Targeting key enzymes, such as tubulin and lipoxygenase, may yield new strategies to impede tumor growth and enhance treatment efficacy.
Objectives: This study aimed to evaluate the anticancer effects of 1,3-thiazole derivatives on A549 and HT-29 cancer cell lines and investigate their ability to inhibit tubulin and lipoxygenase enzymes.
Methods: Ethyl and methyl derivatives with a central 1,3-thiazole core were synthesized in one step. A549 and HT-29 cells were cultured in RPMI 1640 medium. The cytotoxic effects of the derivatives were assessed by treating the cells with varying concentrations for 24, 48, and 72 hours, followed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assays. Molecular docking using AutoDock Vina software, version 1.1.2 was performed to evaluate the derivatives’ inhibitory effects on tubulin and lipoxygenase.
Results: Compound A demonstrated significant anticancer activity against A549 cells at 500 µg/mL. Compound B also inhibited 50% of cancer cells at 1000 µg/mL. In the HT-29 cell line, compound A reduced cell viability by 50% at 500 µg/mL, while compound B showed stronger effects at the same concentration. Ligand A exhibited notable inhibitory potential against tubulin, whereas ligand B had significant inhibitory effects against tubulin and lipoxygenase.
Conclusion: The ethyl substituent of the 1,3-thiazole core shows promise as an anticancer agent against A549, while the methyl substituent is effective against HT-29. Both derivatives can inhibit tubulin function.