α,β-unsaturated compounds derived from arylamines as possible new treatment against leukemia

6^th World Congress on Medicinal Chemistry and Drug Design

June 07-08, 2017 Milan, Italy

Sanchez-Labastida Luis Angel, Bribiesca-Carlos Jose, Andrade-Jorge Erik, Vasquez-Moctezuma Ismael and Trujillo-Ferrara Jose Guadalupe

National Polytechnic Institute, M�©xico

Scientific Tracks Abstracts: Med Chem (Los Angeles)

Abstract :

L5178 cells are an experimental lymphocytic leukemia in mice, associated with hyperplasia of the lymphoid tissues and a high number of circulating malignant lymphocytes and lymphoblast, this cellular line was used to evaluate the activity of a maleimide and a maleimide of phenethylamine, as a possible new treatment for leukemia. Previous studies have shown that �±, �²-unsaturated compounds have important pharmacological properties, as an anti-tumoral activity, this through reducing glutathione levels and increasing oxidative stress, causing cytotoxicity, reduced viability, and death by apoptosis. As the first step, �±, �²-unsaturated compounds were designed from phenylethylamine, the two best candidates were selected. New green synthesis techniques were designed for both compounds and were synthesized, the chemical structure and purity were confirmed by NMR 1H and 13C, mass spectrometry and IR. The compounds were tested in an in vitro experiment with L5178-Y cell culture (50,000 cells approximately per well), treated with the compounds at concentrations of 1x10-3 to 1x10-9 M in both cases. Maleimide derivative showed an activity on cells in concentrations of 1x10-6 to 1x10-4 M, evidenced by the MTT assay at 24 and 48 hours, after that, the field was opened at a concentration between 1x10-6 to 10x10-6 M, and an EC50 of 5x10-6 was obtained. For the case of maleimide, an activity was observed at 1x10-3 to 1x10-5 M, and the open field between 1x10-5 to 1x10-4 M showed an EC50 of 3x10-5 M. The experiment results lead us the possibility to evaluate these compounds in an in vivo models such as survival experiments or LD50 in mice.

Biography :

Sánchez-Labastida Luis Angel is a third year Medical student at Escuela Superior de Medicina of Instituto Politécnico Nacional. In 2013, he started working in the Department of Molecular Biology, and in 2015, in the Biochemistry department, searching for possible treatments against cancer.

Email: langelsl96@gmail.com