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Acta Pharmaceutica, Vol. 63 No. 3, 2013.

Izvorni znanstveni članak
https://doi.org/10.2478/acph-2013-0028

Synthesis, in vitro anticancer and antioxidant activity of thiadiazole substituted thiazolidin-4-ones

ALEX JOSEPH ; Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, India
CHAITANYAKUMAR S. SHAH ; Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, India
SUTHAR SHARAD KUMAR ; Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, India
ANGEL TREASA ALEX ; Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, India
NASEER MALIYAKKAL ; Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, India
SUDHEER MOORKOTH ; Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, India
JESSY ELIZABETH MATHEW ; Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, India

Puni tekst: engleski, pdf (117 KB) str. 397-408 preuzimanja: 963* citiraj
APA 6th Edition
JOSEPH, A., SHAH, C.S., KUMAR, S.S., ALEX, A.T., MALIYAKKAL, N., MOORKOTH, S. i MATHEW, J.E. (2013). Synthesis, in vitro anticancer and antioxidant activity of thiadiazole substituted thiazolidin-4-ones. Acta Pharmaceutica, 63 (3), 397-408. https://doi.org/10.2478/acph-2013-0028
MLA 8th Edition
JOSEPH, ALEX, et al. "Synthesis, in vitro anticancer and antioxidant activity of thiadiazole substituted thiazolidin-4-ones." Acta Pharmaceutica, vol. 63, br. 3, 2013, str. 397-408. https://doi.org/10.2478/acph-2013-0028. Citirano 23.02.2019.
Chicago 17th Edition
JOSEPH, ALEX, CHAITANYAKUMAR S. SHAH, SUTHAR SHARAD KUMAR, ANGEL TREASA ALEX, NASEER MALIYAKKAL, SUDHEER MOORKOTH i JESSY ELIZABETH MATHEW. "Synthesis, in vitro anticancer and antioxidant activity of thiadiazole substituted thiazolidin-4-ones." Acta Pharmaceutica 63, br. 3 (2013): 397-408. https://doi.org/10.2478/acph-2013-0028
Harvard
JOSEPH, A., et al. (2013). 'Synthesis, in vitro anticancer and antioxidant activity of thiadiazole substituted thiazolidin-4-ones', Acta Pharmaceutica, 63(3), str. 397-408. doi: https://doi.org/10.2478/acph-2013-0028
Vancouver
JOSEPH A, SHAH CS, KUMAR SS, ALEX AT, MALIYAKKAL N, MOORKOTH S i sur. Synthesis, in vitro anticancer and antioxidant activity of thiadiazole substituted thiazolidin-4-ones. Acta Pharm. [Internet]. 2013 [pristupljeno 23.02.2019.];63(3):397-408. doi: https://doi.org/10.2478/acph-2013-0028
IEEE
A. JOSEPH, et al., "Synthesis, in vitro anticancer and antioxidant activity of thiadiazole substituted thiazolidin-4-ones", Acta Pharmaceutica, vol.63, br. 3, str. 397-408, 2013. [Online]. doi: https://doi.org/10.2478/acph-2013-0028

Sažetak
A series of novel 5-alkyl/aryl thiadiazole substituted thiazolidin-4-ones were synthesized by a two-step process. In the first step, 5-alkyl/aryl substituted 2-amino-thiadiazoles were synthesized, which on reaction with substituted aromatic aldehydes and thioglycolic acid in presence of dicyclohexylcarbodiimide afforded thiazolidin-4-ones. All compounds were synthesized in fairly good yields and their structures were confirmed by spectral and physical data. The title compounds were screened for in vitro anti-proliferative activity on human breast adenocarcinoma cells (MCF-7) by the MTT assay. Most derivatives showed an IC50 less than 150 µmol L–1. Among the compounds tested, 2-(2-nitrophenyl)-3-(5-methyl-1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3f), 2-(3-fluorophenyl)-3-(5-methyl-1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3b), and 2-(4-chlorophenyl)-3-(5-methyl-1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3c) were found to be the most active derivatives with IC50 values of 46.34, 66.84, and 60.71 µmol L–1, respectively. Antioxidant studies of all synthesized compounds were carried out using diphenylpicrylhydrazyl assay. Among the compounds tested, 2-phenyl-3-(5-styryl-1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3s) elicited superior antioxidant activity with IC50 of 161.93 µmol L–1.

Ključne riječi
thiadiazole; thiazolidin-4-ones; anticancer; antioxidant

Hrčak ID: 102031

URI
https://hrcak.srce.hr/102031

Posjeta: 1.126 *