Design, Synthesis, and Cytotoxic Activities of Indole and Indazole-Based Stilbenes.
Chem Biodivers
; 20(5): e202300368, 2023 May.
Article
em En
| MEDLINE
| ID: mdl-36996024
ABSTRACT
To develop new highly effective anticancer agents derived from naturally occurring stilbene scaffold, in total of 24 indole and indazole-based stilbenes including 17 new compounds were designed according to molecular hybridization strategy and synthesized via Witting reaction. The cytotoxic screening results against human tumor cell lines (K562 cells and MDA-MB-231 cells) showed that indole and indazole-based stilbenes are of great interest for developing anticancer agents as eight derivatives possessed strong antiproliferative activities with IC50 values less than 10â
µM, and those synthetic derivatives displayed more higher cytotoxicities against K562 cells than MDA-MB-231 cells. In particular, indole-based stilbene bearing piperidine exhibited the most potent cytotoxicities against both K562 and MDA-MB-231 cells with IC50 values 2.4â
µM and 2.18â
µM, respectively, along with a remarkable selectivity towards human normal L-02 cells. Together, the results suggested that indole and indazole-based stilbenes are promising anticancer scaffolds worthy of further investigation.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Limite:
Humans
Idioma:
En
Ano de publicação:
2023
Tipo de documento:
Article