Synthesis and investigations into the anticancer and antibacterial activity studies of β-carboline chalcones and their bromide salts.

Basic Information

ID: ALA4219171

Journal: Bioorg Med Chem Lett

Title: Synthesis and investigations into the anticancer and antibacterial activity studies of β-carboline chalcones and their bromide salts.

Authors: Venkataramana Reddy PO, Hridhay M, Nikhil K, Khan S, Jha PN, Shah K, Kumar D.

Abstract: A series of sixteen β-carbolines, bearing chalcone moiety at C-1 position, were prepared from easily accessible 1-acetyl-β-carboline and various aldehydes under basic conditions followed by N2-alkylation using different alkyl bromides. The prepared compounds were evaluated for in vitro cytotoxicity against a panel of human tumor cell lines. N2-Alkylated-β-carboline chalcones 13a-i represented the interesting anticancer activities compared to N2-unsubstituted β-carboline chalcones 12a-g. Off the prepared β-carbolines, 13g exhibited broad spectrum of activity with IC50 values lower than 22.5 µM against all the tested cancer cell lines. Further, the N2-alkylated-β-carboline chalcone 13g markedly induced cell death in MDA-MB-231 cells by AO/EB staining assay. The most cytotoxic compound 13g possessed a relatively high drug score of 0.48. Additionally, the prepared β-carboline chalcones displayed moderate antibacterial activities against tested bacterial strains.

CiteXplore: 29573910

DOI: 10.1016/j.bmcl.2018.03.033

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