Synthesis of 1,3,4-Thiadiazole Derivatives and Their Anticancer Evaluation
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Published:2023-12-14
Issue:24
Volume:24
Page:17476
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ISSN:1422-0067
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Container-title:International Journal of Molecular Sciences
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language:en
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Short-container-title:IJMS
Author:
Stecoza Camelia Elena1, Nitulescu George Mihai1ORCID, Draghici Constantin2, Caproiu Miron Teodor2, Hanganu Anamaria2ORCID, Olaru Octavian Tudorel1ORCID, Mihai Dragos Paul1, Bostan Marinela3ORCID, Mihaila Mirela3ORCID
Affiliation:
1. Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia Street, 020956 Bucharest, Romania 2. “Costin D. Neniţescu” Institute of Organic and Supramolecular Chemistry, Romanian Academy, 202B Splaiul Independenţei, 060023 Bucharest, Romania 3. Stefan S. Nicolau Institute of Virology, 285 Mihai Bravu Street, 030304 Bucharest, Romania
Abstract
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 IC50 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.
Subject
Inorganic Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Computer Science Applications,Spectroscopy,Molecular Biology,General Medicine,Catalysis
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