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Discovery of novel β-carboline/acylhydrazone hybrids as potent antitumor agents and overcome drug resistance.

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Twenty-four novel β-carboline/acylhydrazone hybrids were synthesized and evaluated for their in vitro antiproliferative activity. Among them, 12r exhibited the most potent activity, with IC50 values of 1-2 μM against panel of cancer… Click to show full abstract

Twenty-four novel β-carboline/acylhydrazone hybrids were synthesized and evaluated for their in vitro antiproliferative activity. Among them, 12r exhibited the most potent activity, with IC50 values of 1-2 μM against panel of cancer cell lines and retained significant activity in multidrug resistant cancer cells. Treated cells were not arrested in any phase of cell cycle but resulted in late cellular apoptosis on both MCF-7 and MCF-7/ADR cancer cells. Importantly, 12r showed certain antitumor effect on inhibiting the tumor growth with low toxic and side effects and without significant body weight loss.

Keywords: novel carboline; acylhydrazone hybrids; discovery novel; carboline acylhydrazone

Journal Title: European journal of medicinal chemistry
Year Published: 2018

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