Plenary Lecture 10



Title: Nature-mimetic small molecules: From the land, from the sea,
from the lab and through the looking-glass…

Professor Madalena M. M. Pinto

University of Porto/CIIMAR, Portugal
 

 

During some decades the main goal of our research group has been dedicated to the synthesis and molecular modification of nature-mimetic compounds (xanthone/flavonoid/polyphenol scaffolds), predominantly in an interdisciplinary way, comprising of Organic Chemistry, Biology, Computer-aided Design, X-Ray Crystallography and Drug Delivery Systems, including multi active ligands with cell growth inhibitory effects, P-gp1, caspases2 and p53/MDM2 modulation3, as well as new anticoagulants4 and agents for artificial chiral molecular recognition. The integration of our research group in CIIMAR was an inflection point that opened a new wave of strategy models for new small molecule collections as well as structure-activity data.

Here the evolution of the work carried out by our research group based on natural molecules as a toolbox which gives an insight into the diversity of strategies applied to the hit-to-lead optimization process, as well as associated concepts of privileged structures, molecular hybridization, structure-based design, among others, is disclosed. The research that is currently being developed relating to the discovery of marine natural products/nature-mimics having as a main target to prevent and/or treat diseases, in particular cancer, neurodegenerative diseases, overweight and obesity, as well as overcoming multidrug resistance 5 is also highlighted.

 

Acknowledgments: Project INNOVMAR—Innovation and Sustainability in the Management and Exploitation of Marine Resources (reference NORTE-01-0145-FEDER-000035, within Research Line NOVELMAR/INSEAFOOD/ECOSERVICES), supported by North Portugal Regional Operational Programme (NORTE 2020), under the PORTUGAL 2020 Partnership Agreement, through the European Regional Development Fund (ERDF).



References: 1 Palmeira, A.; Sousa, E.; Vasconcelos, H.; Pinto, M.; Fernandes, M.X.; Curr. Pharm. Des. 2012, 18, 4197

2 Pereira, C.; Lopes-Rodrigues, V.; Coutinho, I.; Neves, M.; Lima, R.; Pinto, M.; Cidade, H.; Vasconcelos, H.; Saraiva, L., Eur. J. Med. Chem. 2014,54,8-16

3 Lemos, L.; Leão, M.; Soares, J.; Palmeira, A.; Pinto, M.; Saraiva, L.; Sousa,M. E., Med. Res. Rev. 2016, 00, No. 0, 1–56

4 Correia-da-Silva,M.; Sousa, E.; Duarte, B.; Marques, F.; Carvalho, F.; Cunha-Ribeiro, L.; Pinto, M.; J. Med. Chem., 2011, 54(1), 95-106

5Long, S.; Sousa, E.; Kijjoa, A.; Pinto, M., Molecules 2016, 21, 892