title: Cytotoxicity and Antioxidant Potential of Novel 2-(2-((1H-indol-5yl)methylene)-hydrazinyl)-thiazole Derivatives.
abstract: Newly synthesized 2-(2-((1H-indol-5yl)methylene)-hydrazinyl)-thiazole derivatives were evaluated for their in vitro cytotoxicity on two carcinoma cell lines A2780 and HeLa. Significant cytotoxic activity for 2-(2-((1H-indol-5-yl)methylene)hydrazinyl)-4-methylthiazole (1) and 2-(2-((1H-indol-5-yl)methylene)hydrazinyl)-4-phenylthiazole (3), on both A2780 [IC50: 11.6 μM (1), and 12.4 μM (3)] and HeLa [IC50: 22.4 μM (1) and 19.4μM (3)] cell lines is reported. Their antioxidant potential was evaluated by spectrophotometric method, using DPPH radical or Fe (TPTZ)3+complex, and EPR spectroscopy, therefore the compounds1and3showed remarkable antioxidant activity simultaneously with a cytotoxic effect on A2780 and HeLa cell lines. Furthermore, based on theoretical quantum chemical calculation, the present study analyzed the chemoselectivity of the hydrogen extraction from the indolyl-hydrazinil-thiazoles in reaction with free radicals.
authors.affiliation: Department of Organic Chemistry, Faculty of Pharmacy, "Iuliu Haţieganu" University of Medicine and Pharmacy, 8 Victor Babes, Cluj-Napoca RO-400012, Romania. adriana.ignat@umfcluj.ro.
authors.forename: Adriana
authors.initials: A
authors.lastname: Grozav
authors.affiliation: Research Center on Fundamental and Applied Heterochemistry, Faculty of Chemistry and Chemical Engineering, "Babeş-Bolyai", University, M. Kogalniceanu 1, Cluj-Napoca RO-400028, Romania. pdan@chem.ubbcluj.ro.
authors.forename: Ioan-Dan
authors.initials: ID
authors.lastname: Porumb
authors.affiliation: Research Center on Fundamental and Applied Heterochemistry, Faculty of Chemistry and Chemical Engineering, "Babeş-Bolyai", University, M. Kogalniceanu 1, Cluj-Napoca RO-400028, Romania. gluiza@chem.ubbcluj.ro.
authors.forename: Luiza Ioana
authors.initials: LI
authors.lastname: Găină
authors.affiliation: Department of Bromatology, Hygiene, Nutrition, Faculty of Pharmacy, "Iuliu Haţieganu" University of Medicine and Pharmacy, 8 Victor Babes, Cluj-Napoca RO-400012, Romania. lfilip@umfcluj.ro.
authors.forename: Lorena
authors.initials: L
authors.lastname: Filip
authors.affiliation: Department of Pharmacognosy Faculty of Pharmacy, "Iuliu Haţieganu" University of Medicine and Pharmacy, 8 Victor Babes, Cluj-Napoca RO-400012, Romania. dhanganu@umfcluj.ro.
authors.forename: Daniela
authors.initials: D
authors.lastname: Hanganu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D005609:Free Radicals / Q000037:antagonists & inhibitors; D006801:Humans; D020128:Inhibitory Concentration 50; D009682:Magnetic Resonance Spectroscopy / Q000379:methods; D008958:Models, Molecular; D008968:Molecular Conformation; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D000975:Antioxidants; D005609:Free Radicals; D013844:Thiazoles
keywords: DFT calculation; antioxidant activity; cytotoxic activity; indol; thiazole