CHIRALBIOACTIVE-PI-3RL-IINFACTS-2019: Chiral derivatives of xanthones and flavonoids: synthesis and biological activity evaluation.

Principal Investigator: 
Maria Elizabeth Tiritan (
Leader Institution: 
Research Team: 
Maria Elizabeth Tiritan (PI), Odília Queirós (Co-PI), Cristina Coelho (Co-PI), Alexandra Costa, Paolo De Marco, Sandra Quinteira, Sónia Marisa Machado, Carla Fernandes, Madalena Pinto, Carlos Afonso, Emilia Sousa, Honorina Cidade, Marta Correia da Silva, Virginia Gonçalves, Helena Susana da Costa Machado Ferreira, Nuno João Meleiro Alves das Neves, Sara Filipa Fontoura Vieira, Hassan Bousbaa, Patrícia Silva, Joel Pedrosa, Andrea Cunha, Juliana Faria, Joana Barbosa, Orquídea Lurdes Alves Resende
Funding entity: 
Period covered: 
03/2019 - 02/2020

Xanthone derivatives and flavonoids demonstrated great potential in diverse biological activities. They are interesting chemical building blocks for preparation of new derivatives with association with chiral moieties allowing to enlarge the chemical diversity and to explore the role of the molecular stereochemistry. This work aim to synthesize a new library of chiral derivatives of xanthones (CDXs) and flavonoids (CDFs) by coupling to enantiomerically pure amino alcohols, amines, proteinogenic amino esters and amino acids. Diverse biological activities of the CDXs and CDFs will be evaluated comprising, anti-inflammatory, anti-infective and antitumor. Resistance to treatment associated with cancer therapy is often caused by the expression of efflux pumps in cancer cells, we will determine if these compounds are P-glycoprotein (Pgp) substrates, by using a MDR1-transformant yeast as host. Furthermore, their effectiveness on tumor cells will be studied through high-throughput assays of viability. As the bioenergetic deregulation is one of the emergent cancer hallmarks, their effect on metabolic parameters like lactate and glucose will also be assessed.


Project area: