Full Professor, Faculdade de Farmácia, Universidade de Lisboa
Program Area Leader, Drug Design at iMed.ULisboa
The group Medicinal Chemistry applies principles and techniques of medicinal chemistry to understand biology and to identify novel and robust chemical starting points for chemical biology and lead optimization. Major objectives of the group include:
– Synthesis of focused chemical libraries for target- and phenotypic cell-based screenings to discover novel lead compounds for cancer and infectious diseases;
– Design and synthesis of selective covalent inhibitors for proteases as diagnostic and therapeutic tools, through modulation of intrinsic reactivity and molecular recognition of novel chemical scaffolds;
– Computational discovery of chemical tools in drug discovery. We develop technically advanced computer-aided drug refinement tools to streamline the hit generation process for cancer and malaria targets;
– Development of prodrugs as chemical drug delivery systems to address selectivity, permeability and chemical/metabolic stability issues commonly found in many drugs and drug candidates.
Recent achievements of the Medicinal Chemistry group at iMed.ULisboa.
Source: FCT (PTDC/BBB-BEP/2463/2014)
Title: ProbeCOPD. Protease activity-based probes for Chronic Obstructive Pulmonary Disease diagnostics
PI: Rui Moreira
Source: FCT (PTDC/QEQ-MED/7042/2014)
Title: Small-molecule inhibitors of human proteasome: a step forward in anticancer drug discovery
PI: Rita Guedes
Source: FCT (PTDC/QEQ-MED/7097/2014)
Title: Exploring TOR/PI3K kinases as targets for treating protozoan neglected tropical diseases
PI: Ana Ressurreição
Source: ERANET and FCT (ENMed/0051/2016)
Title: Modulation of melanoma-stroma interactions using a rationally-designed nanomedicine combining BRAFi-, MEKi- and immune-therapies
PI: Helena Florindo
Source: COMPETE2020 and FCT (SAICTPAC/0019/2015)
Title: POINT4PAC – Precision Oncology by Innovative Therapies and Technologies
PI: Cecília M. P. Rodrigues
Recent Most Relevant Publications
Pinheiro R, Braga C, Santos G, Bronze MR, Perry MJ, Moreira R, Brites D, Falcão AS. Targeting gliomas: can a new alkylating hybrid compound make a difference? ACS Chem Neurosci 2017; 8: 50-59.
Soares J, Espadinha M, Raimundo L, Ramos H, Gomes AS, Gomes S, Loureiro JB, Inga A, Reis F, Gomes C, Santos MMM, Saraiva L. DIMP53-1: A novel small-molecule dual inhibitor of p53-MDM2/X interactions with multifunctional p53-dependent anticancer properties. Molecular Oncology 2017; 11: 612-27.
Bonito CA, Nunes J, Leandro J, Louro F, Leandro P, Ventura FV, Guedes RC. Unveiling the Pathogenic Molecular Mechanisms of the Most Common Variant (p.K329E) in Medium-Chain Acyl-CoA Dehydrogenase Deficiency by in Vitro and in Silico Approaches. Biochemistry 2016; 55: 7086-98
Lavrado J, Brito H, Borralho PM, Ohnmacht SA, Kim NS, Leitão C, Pisco S, Gunaratnam M, Rodrigues CMP, Moreira R, Neidle S, Paulo A. KRAS oncogene repression in colon cancer cell lines by G-quadruplex binding indolo[3,2-c]quinolines. Sc Rep 2015; 5: 9696.
Oliveira R, Guedes RC, Meireles P, Albuquerque IS, Gonçalves LM, Pires E, Bronze MR, Gut J, Rosenthal PJ, Prudêncio M, Moreira R, O’Neill PM, Lopes F. Tetraoxane-Pyrimidine Nitrile Hybrids as Dual Stage Antimalarials. J Med Chem. 2014; 57: 4916-23.
Full Professor T +351 217 946 400 (Ext. 14381)
- Andreia Figueiredo
- Andreia Gonçalves
- Daniela Coutinho
- Dário Silva
- Elizabeth Lopes
- Joana Ribeiro
- Ana Rita Felix
- Lara Fidalgo
- Pedro Fernandes
- Valentina Barcherini