Isoindolines as potential modulators of human histone deacetylase: New discovery

4^th International Conference on Medicinal Chemistry & Computer Aided Drug Designing

November 02-04, 2015 Atlanta, USA

Jos�© Bribiesca Carlos, Erik Andrade Jorge, Jos�© Guadalupe Trujillo Ferrara, Ernesto Daniel Guevara Avenda�±o and Luis Daniel Manzano Ruiz

Instituto Polit�©cnico Nacional, M�©xico

Posters-Accepted Abstracts: Med chem

Abstract :

Cancer is a disease that is taking great importance in societies worldwide, so that has been earmarked much of the worldâ��s resources in finding an effective treatment. Currently, it is intended that new anticancer drugs to be more selective and do not generate side effects. This has been possible with new technologies that allow us to develop drugs with high selectivity to act at a specific level by inhibiting important processes in the cancer cells. The aim of this work was to develop a series of isoindolines as inhibitors of HDAC (Histone Deacetylase), a key enzyme in the transcription of genetic information; the purpose of these ligands is inhibition of histone deacetylase leading to a hyper-acetylation state to allow transcription of anti-oncogenes like NF�ºB, p53, Ku70, tubulin, among others. The results demonstrate that our compound decreases cell viability at the concentration of 1x10-3 M at 24 and 48 hours, the results were obtained by two methods: through spectroscopy at 540 nm and cell counting performed by a cell counter. The compound decreased the cell viability 50% at 24 hours and 20% at 48 h (p<0.05). In spite of these excellent results we found a second effect that is related with cell proliferation at concentrations lower than 1x10-7 M, setting a new question on the table: what is the mechanism of this biphasic effect? Therefore, it is necessary research in different cell lines to test their proliferative effect and its possible applications.