NDLI: A novel class of piperidones exhibit potent, selective and pro-apoptotic anti-leukemia properties

Content Provider	PubMed Central
Author	Nunes, Larissa M. Hossain, Md Armando, Varela-ramirez Das, Umashankar Ayala-marin, Yoshira M. Dimmock, Jonathan R. Aguilera, Renato J.
Copyright Year	2016
Abstract	In the present pre-clinical study, a series of 1-[3-(2-methoxyethylthio)-propionyl]-3,5- bis(benzylidene)-4 piperidones and structurally-related compounds were observed to be cytotoxic in vitro to three human leukemia cell lines, namely Nalm-6, CEM and Jurkat. The 50% cytotoxic concentration (CC50) values of the three cell lines ranged between 0.9–126.4 µM and 0.3–11.7 µM at 24 and 48 h subsequent to exposure, respectively. The two lead compounds with sub-micromolar CC50 concentrations, 1-(2-methoxyethylthio-propionyl)-3,5-bis(benzylidene)-4 piperidone (2a) and 3,5-bis(4-fluorobenzylidene)-1-[3-(2-methoxyethyl sulfinyl)-propionyl]-4-piperidone (3e), were selected for additional analyses. Several strategies were undertaken to determine whether the above piperidones caused cell death via apoptosis or necrosis on T-lymphocyte leukemia Jurkat cells. The results revealed that the two piperidones caused phosphatidylserine externalization, mitochondrial depolarization and activation of caspase-3, which are all biochemical hallmarks of apoptosis. In addition, the selected piperidones displayed selective cytotoxicity towards leukemia cells, and were less toxic in non-cancerous control cells. Therefore, the findings of the present study revealed that the novel piperidones 2a and 3e exert a selective cytotoxic effect on lymphocyte leukemia cells by favoring the activation of the intrinsic/mitochondrial apoptotic pathway.
Related Links	http://dx.doi.org/10.3892/ol.2016.4480
Starting Page	3842
File Format	PDF
ISSN	17921074
e-ISSN	17921082
Journal	Oncology Letters
Issue Number	6
Volume Number	11
Language	English
Publisher	D.A. Spandidos
Publisher Date	2016-04-01
Access Restriction	Open
Rights Holder	D.A. Spandidos
Subject Keyword	Cancer Research Oncology Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	Cancer Research Oncology

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