Synthesis of some novel 2-substituted-[1,3]thiazolo[3,2-a]benzimidazol-3(2h)-ones as potent cytostatic agents
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2016-01-01
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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.