Synthesis of 1,3,4-Thiadiazole Derivatives and Their Anticancer Evaluation.
Camelia Elena StecozaGeorge Mihai NițulescuConstantin DraghiciMiron Teodor CaproiuAnamaria HanganuOctavian Tudorel OlaruDragos Paul MihaiMarinela BostanMirela Antonela MihailaPublished in: International journal of molecular sciences (2023)
Thiadiazole derivatives have garnered significant attention in the field of medicinal chemistry due to their diverse pharmacological activities, including anticancer properties. This article presents the synthesis of a series of thiadiazole derivatives and investigates their chemical characterization and potential anticancer effects on various cell lines. The results of the nuclear magnetic resonance (NMR) analyses confirmed the successful formation of the target compounds. The anticancer potential was evaluated through in silico and in vitro cell-based assays using LoVo and MCF-7 cancer lines. The assays included cell viability, proliferation, apoptosis, and cell cycle analysis to assess the compounds' effects on cancer cell growth and survival. Daphnia magna was used as an invertebrate model for the toxicity evaluation of the compounds. The results revealed promising anticancer activity for several of the synthesized derivatives, suggesting their potential as lead compounds for further drug development. The novel compound 2g , 5-[2-(benzenesulfonylmethyl)phenyl]-1,3,4-thiadiazol-2-amine, demonstrated good anti-proliferative effects, exhibiting an IC 50 value of 2.44 µM against LoVo and 23.29 µM against MCF-7 after a 48-h incubation and little toxic effects in the Daphnia test.
Keyphrases
- cell cycle
- magnetic resonance
- papillary thyroid
- oxidative stress
- single cell
- cell proliferation
- structure activity relationship
- high throughput
- squamous cell
- breast cancer cells
- high resolution
- cell death
- young adults
- mesenchymal stem cells
- stem cells
- squamous cell carcinoma
- endoplasmic reticulum stress
- computed tomography
- childhood cancer
- contrast enhanced
- clinical evaluation