Synthesis and antitumor activity of novel N-substituted tetrahydro-ß-carboline-imidazolium salt derivatives.
Org Biomol Chem
; 14(39): 9423-9430, 2016 Oct 04.
Article
em En
| MEDLINE
| ID: mdl-27714171
ABSTRACT
The synthesis of a series of novel N-substituted tetrahydro-ß-carboline-imidazolium salt derivatives is presented. The biological properties of the compounds were evaluated in vitro against a panel of human tumor cell lines. The results suggest that the benzimidazole ring and 1-(naphthalen-2-yl)ethan-1-one or 2-naphthylmethyl substituent at the imidazolyl-3-position were vital for modulating cytotoxic activity. Compound 41 was observed as a potent derivative with IC50 values of 3.24-8.78 µM and exhibited cytotoxic activity selectively against HL-60, A-549 and MCF-7 cell lines. Meanwhile, high inhibitory activities selectively against HL-60 and MCF-7 cell lines were observed for compound 51. Moreover, compound 51 was able to induce G1 phase cell cycle arrest and apoptosis in MCF-7 cells. The cytotoxicity of compound 51 against human normal lung epithelial cell line BEAS-2B was further evaluated.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Imidazóis
/
Antineoplásicos
Limite:
Humans
Idioma:
En
Ano de publicação:
2016
Tipo de documento:
Article