Mavrova A.Wesselinova D.Anichina K.2024-07-162024-07-162024-07-162024-07-162016-01-011314-79781314-7471SCOPUS_ID:84994274805https://rlib.uctm.edu/handle/123456789/1152An 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.enArticle