Kumar, Sujeet ; Hegde, Mahesh ; Gopalakrishnan, Vidya ; Renuka, Vinaya Kumar ; Ramareddy, Sureshbabu A. ; De Clercq, Erik ; Schols, Dominique ; Gudibabande Narasimhamurthy, Anil Kumar ; Raghavan, Sathees C. ; Karki, Subhas S. (2014) 2-(4-Chlorobenzyl)-6-arylimidazo [2, 1-b][1, 3, 4] thiadiazoles: synthesis, cytotoxic activity and mechanism of action European Journal of Medicinal Chemistry, 84 . pp. 687-697. ISSN 0223-5234
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Official URL: http://www.sciencedirect.com/science/article/pii/S...
Related URL: http://dx.doi.org/10.1016/j.ejmech.2014.07.054
Abstract
The cytotoxic activity of a new series of 2-(4′-chlorobenzyl)-5,6-disubstituted imidazo[2,1-b][1,3,4]thiadiazoles against different human and murine cancer cell lines is reported. Among the tested compounds, two derivatives namely 2-(4-chlorobenzyl)-6-(2-oxo-2H-chromen-3-yl)imidazo[2,1-b][1,3,4]thiadiazole-5-carbaldehyde 4i and 2-(4-chlorobenzyl)-6-(2-oxo-2H-chromen-3-yl)imidazo[2,1-b][1,3,4]thiadiazol-5-yl thiocyanate 5i emerged as the most potent against all the cell lines. To investigate the mechanism of action, we selected compounds 4i for cell cycle study, analysis of mitochondrial membrane potential and Annexin V-FITC flow cytometric analysis and DNA fragmentation assay. Results showed that 4i induced cytotoxicity by inducing apoptosis without arresting the cell cycle.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to Elsevier Science. |
| Keywords: | Anti-cancer Drugs; Cancer Therapeutics; Cytotoxicity; Apoptosis; Cell Death |
| ID Code: | 104074 |
| Deposited On: | 07 Apr 2017 07:01 |
| Last Modified: | 07 Apr 2017 10:13 |
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