Synthesis of some novel 2-substituted-[1,3]thiazolo[3,2-a]benzimidazol-3(2h)-ones as potent cytostatic agents
| creativework.keywords | Anticancer activity, Cells proliferation, MTS test, Thiazolobenzimidazolones | |
| creativework.publisher | University of Chemical Technology and Metallurgyjournal@uctm.edu | en |
| dc.contributor.author | Mavrova A. | |
| dc.contributor.author | Wesselinova D. | |
| dc.contributor.author | Anichina K. | |
| dc.date.accessioned | 2024-07-16T11:16:47Z | |
| dc.date.accessioned | 2024-07-16T11:18:25Z | |
| dc.date.available | 2024-07-16T11:16:47Z | |
| dc.date.available | 2024-07-16T11:18:25Z | |
| dc.date.issued | 2016-01-01 | |
| dc.description.abstract | An optimized method for the synthesis of new 2-substituted-thiazolo[2,3-a]benzimidazole-3(2H)-ones was developed which enabled the target compounds to be obtained in relative good yields through one pot process.Four cancer cell lines: human colorectal cancer cell line HT-29, breast cancer cells MDA-MB-231, cervical cancer cells HeLa, human liver carcinoma cell line HepG2 and human diploid cell line Lep-3 were used to estimate the effects of the newly synthesized compounds on cell proliferation. The initial biological screening in vitro, using MTS tetrazolium assay showed that the tested thiazolobenzimidazolones (compounds 7 and 11) demonstrated selective cytotoxicity against HT-29 cells (IC50 - 3.5.10-2 μM and IC50 - 5.0.10-2 μM, respectively), while compound 9 manifested selective cytotoxicity against Hep G2. Beside that the compounds 9 and 11 induced proliferation activity towards Lep3 cells at extremely low concentrations. EC50 values were 3.4.10-2 μM and 1.410-2 μM, correspondingly. The activity results towards HT-29 and Hep G2 cells indicated the necessity for further investigation in vivo to estimate the exact inhibition pathway of the cellular processes. | |
| dc.identifier.issn | 1314-7978 | |
| dc.identifier.issn | 1314-7471 | |
| dc.identifier.scopus | SCOPUS_ID:84994274805 | en |
| dc.identifier.uri | https://rlib.uctm.edu/handle/123456789/1152 | |
| dc.language.iso | en | |
| dc.source.uri | https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=84994274805&origin=inward | |
| dc.title | Synthesis of some novel 2-substituted-[1,3]thiazolo[3,2-a]benzimidazol-3(2h)-ones as potent cytostatic agents | |
| dc.type | Article | |
| oaire.citation.issue | 6 | |
| oaire.citation.volume | 51 |