cancer-therapy-and-biomarkers-2016_tracks-abstracts

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Volume 2, Issue 3(Suppl) Oncol Cancer Case Rep
ISSN: 2471-8556 an open access journal
Page 26
Notes:
Cancer Therapy & Biomarkers 2016
December 05-07, 2016
conferenceseries.com
CANCER THERAPY,
BIOMARKERS & CLINICAL RESEARCH
15th World Congress on
December 05-07, 2016 Philadelphia, USA
Phenylethyl maleimide derivatives as novel apoptosis inducers on L5178-Y murine leukemia cells
(in silico, in vitro and in vivo study)
Erik Andrade Jorge and José Guadalupe Trujillo Ferrara.
Escuela Superior de Medicina, Instituto Politécnico Nacional, México
C onventional cancer therapies have been shown to have many side effects, the main challenge is to find molecules with high-
er selectivity to tumor cells rather than normal cells. A main differences between cancer and normal cells, are the levels of
thiol-containing compounds, a scavenging mechanism of Reactive Oxygen Species. Cancer cells seem to have higher levels of
glutathione than normal cells, and this allow them to survive in adverse conditions, even in chemotherapy. Therefore, glutathi-
one has become a target for the new anticancer therapy. The aim of this contribution was to develop a series of α,β-unsaturated
compounds derivate of endogenous amines that may deplete the levels of glutathione, as well as, induce cancer cells to death by
apoptosis. Pharmacokinetic evaluation (in silico) showed a good score on the the parameters such as human intestinal absorp-
tion, plasma protein binding, biotransformation evaluated by cytochrome CYP2C9 affinity and CYP2D6 affinity, P-glycopro-
tein substrate, LopP, etc. The in vitro assays showed a EC50 of 5µM for molecule MF01 and a EC50 of 30 µM for molecule MF02
evaluated by MTT method at 24 and 48h, in vivo experiments include LD50 and survival experiment. It was estimated a LD50
for MF01 of 8mg/kg and 80mg/kg for molecule MF02, which means that molecule MF02 is 10 times less toxic that molecule
MF01. There wasn’t significant difference on the survival experiment at the dose used, but there was a delay on the tumor’s
development on the treated group. These results allow us to try others candidates which might possess the same properties.
Biography
Erik Andrade-Jorge is a Doctorate student in the Department of Biochemistry at Instituto Politecnico Nacional. He is a chemist-pharmaceutical-biologist and has a
Master degree in Pharmacology and is currently in the seventh semester of the Doctorate in research in medicine. Currently, he has two different lines research one
of these is cancer cell proliferation and another one is in Parkinson’s disease. He has been focused on the rational drug design based on the molecular mechanisms
of different pathologies and in the physicochemical properties of the ligands.
Erik Andrade Jorge et al., Oncol Cancer Case Rep 2016,2:3(Suppl)