Estrategia de enlace covalente: Síntesis de pirido[2,3-d]primidinas con aceptores de Michael como potenciales agentes anticáncer


Mora Obea, Óscar


Cancer is caused by a deregulation of cells where kinases are generally associated. Cancer treatments can be very diverse and in the recent years have been developed new ones, such as targeted therapy.
Since kinases are present in most cancer processes, they have become one of the main targets for targeted therapies. This treatment reduces off-target reactivity so that toxicity is lower than traditional chemotherapeutics.
There are different inhibitory structures of this enzyme which, depending on their structure, can bind reversibly or irreversibly to the active site. Currently, irreversible covalent inhibitors have advantages over other reversible and non-covalent treatments. Acrylamides are an example of irreversible tyrosine kinase inhibitors, where their mechanism of inhibition is via Michael acceptors.
In this work, an intention is to synthesize a potential irreversible tyrosine kinase inhibitory agent with a Michael acceptor in its structure. Also, an improvement of this formulation is tried by adding a substructure that can provide better pharmacokinetic properties to the final product.



Puig de la Bellacasa Cazorla, Raimon


IQS SE - Undergraduate Program in Pharmacy