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Synthesis and biological assessment of indole derivatives containing penta-heterocycles scaffold as novel anticancer agents towards A549 and K562 cells. | LitMetric
Herein, a new series of 2-chloro--(5-(2-oxoindolin-3-yl)-4-pyrazol-3-yl) acetamide derivatives containing 1,3,4thiadiazole () and 4-1,2,4-triazol-4-amine () moiety was designed, synthesised as novel anticancer agents. The antiproliferative activity values indicated that compound stood as the most potent derivative with IC values of 12.0 nM and 10 nM against A549 and K562 cells, respectively. Mechanism investigation and docking studies of indicated that it possessed good apoptosis characteristic and dose-dependent growth arrest of A549 and K562 cells, blocked cell cycle into G2/M phase. Interestingly, suppressed the growth of A549 and K562 cells via modulation of EGFR and p53-MDM2 mediated pathway.
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