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

ABSTRACT: A series of sixteen ?-carbolines, bearing chalcone moiety at C-1 position, were prepared from easily accessible 1-acetyl-?-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-?-carboline chalcones 13a-i represented the interesting anticancer activities compared to N2-unsubstituted ?-carboline chalcones 12a-g. Off the prepared ?-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-?-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 ?-carboline chalcones displayed moderate antibacterial activities against tested bacterial strains.

SUBMITTER: Venkataramana Reddy PO 

PROVIDER: S-EPMC6423518 | biostudies-literature | 2018 May

REPOSITORIES: biostudies-literature

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

Venkataramana Reddy P O PO   Hridhay M M   Nikhil Kumar K   Khan Shahid S   Jha P N PN   Shah Kavita K   Kumar Dalip D  

Bioorganic & medicinal chemistry letters 20180313 8

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 N<sup>2</sup>-alkylation using different alkyl bromides. The prepared compounds were evaluated for in vitro cytotoxicity against a panel of human tumor cell lines. N<sup>2</sup>-Alkylated-β-carboline chalcones 13a-i represented the interesting anticancer activities compared to N<sup>2</sup>-unsubstituted β-ca  ...[more]

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