Synthesis and potent antileukemic activities of 10-benzyl-9(10H)-acridinones

Bioorganic & Medicinal Chemistry
Chunmei GaoDerong Cao

Abstract

A novel series of 10-benzyl-9(10H)-acridinones and 1-benzyl-4-piperidones were synthesized and tested for their in vitro antitumor activities against CCRF-CEM cells. Assay-based antiproliferative activity study using CCRF-CEM cell lines revealed that the acridone group and the substitution pattern on the benzene unit had significant effect on cytotoxicity of this series of compounds, among which 10-(3,5-dimethoxy)benzyl-9(10H)-acridinone (3b) was found to be the most active compound with IC(50) at about 0.7 microM. Compound 3b was also found to have antiproliferative activity against two other human leukemic cell lines K562 and HL60 using the MTT assay. The antitumor effect of 3b is believed to be due to the induction of apoptosis, which is further confirmed by PI (Propidium iodide) staining and Annexin V-FITC/PI staining assay using flow cytometry analysis.

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Citations

Apr 12, 2012·Environmental Science & Technology·Charles E West, Steven J Rowland
Oct 19, 2012·Journal of Medicinal Chemistry·Victor Hernandez-OlmosChrista E Müller
Mar 29, 2014·TheScientificWorldJournal·Thankarajan Sajeesh, Thangaraj Parimelazhagan
May 20, 2014·Chembiochem : a European Journal of Chemical Biology·Xiangqian LiZhichao Zhang
Feb 24, 2016·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Huda S KareemAzhar Ariffin

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Apoptosis

Apoptosis is a specific process that leads to programmed cell death through the activation of an evolutionary conserved intracellular pathway leading to pathognomic cellular changes distinct from cellular necrosis