Karabulut, H. R. FerhatKaratavuk, Ali OsmanOzyildirim, HasanDoganlar, OguzhanDoganlar, Zeynep Banu2024-06-122024-06-1220201054-25231554-8120https://doi.org/10.1007/s00044-020-02510-xhttps://hdl.handle.net/20.500.14551/19865In this study, the main aim was synthesis of dimeric compounds, which contain lithocholic acid and a triazole structure to investigate the selective cellular and molecular antiproliferative and proapoptotic potential of these products in healthy embryonic fibroblast (MEF), cervix cancer (HeLa), and breast cancer (MCF-7) cells. Four ester (5a-d) and five dimeric (6a-d, 7) out of nine novel compounds were obtained. First of all, lithocholic acid was converted to methyl lithocholate and then it was reacted with certain alkynoic acids (a-d) to obtain its alkynoate derivatives (5a-d). Finally, these compounds were converted to dimers (6a-d) by using 2,6-bis(azidomethyl)pyridine via the click method. Our result indicate that, treatment with dimeric compounds can selectively decrease the cell viability and proliferation in cervix cancer HeLa and breast cancer MCF-7 cells, except 7 which caused a strong cytotoxicity on healthy MEF cells. According to MTT assay, Nucblue cell stain and Annexin V/Propodium iodide molecular probe staining, 100 mu M concentrations of the dimeric compounds was sufficient in inducing death and apoptotic cell ratio in HeLa and MCF-7 breast cancer cells selectively. In brief, the present study indicates that most effective dimeric compounds are 6a and 6b, which have the highest IC50 (345.8-342.6 mu M) value on healthy cell and the lowest IC50 value in both cervix (49.2-36.9 mu M) and breast (23.0-66.1 mu M) cancer cells especially long-term treatment and which triggers apoptosis pathway specifically.en10.1007/s00044-020-02510-xinfo:eu-repo/semantics/closedAccessClick ChemistryLithocholic AcidHelaMCF-7Gene ExpressionLithocholic AcidDerivativesChemistryActivationTherapyAnalogsDesignCellsHivArticle294643655Q4WOS:0005207066000052-s2.0-85078332082Q2