IQUIR   05412
INSTITUTO DE QUIMICA ROSARIO
Unidad Ejecutora - UE
congresos y reuniones científicas
Título:
Multiple Synthetic Strategies for the Generation of Triazolylpeptidyl Penicillin Analogs in the Search for New Antitumoral Compounds
Autor/es:
MARTIREN, NADIA L.; BLANK, VIVIANA; MATA, ERNESTO G.; BELLIZZI, YANINA; CORNIER, PATRICIA G.; BARRIONUEVO, E.; ROGUIN, LEONOR P.
Lugar:
Pirenópolis
Reunión:
Simposio; 9Th Brazilian Symposium on Medicinal Chemistry; 2019
Institución organizadora:
Divisão de Química Medicinal - Sociedade Brasileira de Química
Resumen:
Cancer therapeutics requires the constant search and development of new and better drugs, due to the resistance phenomena and complexity of this disease. A goal of one of our research lines, is to find answers to this problem through the design, synthesis and analysis of potentially bioactive structures.Employing molecular hybridization methodology and a solid phase organic chemistry approach, we synthesized a library of compounds that conjugate a penicillin derivative to a peptide through a triazole group.These compounds were evaluated as antiproliferative agents in vitro, and several of them showed an outstanding activity and selectivity. Based on the anticancer activity of these triazolylpeptidyl penicillins, we have designed multiple strategies to synthesize new derivatives (figure 1) in order to evaluate the structure-activity relationship, improve the solubility profiles and increase our knowledge of the mechanism of action.