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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

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

doi

10.1016/j.bmcl.2018.03.033

subject

Has Abstract

pub_date

2018-05-01 00:00:00

pages

1278-1282

issue

8

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(18)30222-1

journal_volume

28

pub_type

杂志文章

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