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Marine Natural Products and Medicinal Chemistry

Principal Investigator:
Madalena Pinto

Isolation and structure elucidation of bioactive compounds from marine-derived fungi, marine sponges and marine invertebrates. Production of new specialized metabolites from marine-derived fungi with modification of culture media. Study of absolute configurations of marine-derived chiral molecules by electronic circular dichroism, X-ray crystallography and chiral-phase HPLC. Bioactive secondary metabolites from marine origin with antibacterial, anti-tyrosinase and anti-cholinesterase activities. Synthesis of bioactive novel marine natural products with potential as drug candidates/industrial applications (total synthesis, semi-synthesis, analogue-based design). Structure-based design of potential drug candidates based on marine natural product leads, studies of structure-properties-activity relationships, optimization of bioactive compounds, and preformulation studies. Development of small molecules with low ecotoxicity, (bio)degradable, particularly, antifouling agents and new siderophore/siderophore-mimetic conjugates, as an innovative area to solve environmental problems. Sustainable synthetic procedures and purification methods to reduce negative environmental impacts. Enantiomeric studies on chiral bioactive compounds and their impact on environment. In vitro screening for several biological activities; study of cellular and molecular mechanisms of action of the most promising compounds, namely with targets related to tumorigenesis (mitosis) and inflammation (enzymes of the arachidonic acid cascade) and antimicrobial and antibiofilm activities (strategies for overcoming multidrug-resistance).

 

MNP&MEDCHEM Co-PI: Anake Kijjoa

TEAM

Publications Highlights

Wibowo, J. T., Ahmadi, P., Rahmawati, S. I., Bayu, A., Putra, M. Y., Kijjoa, A. (2022). Marine-derived indole alkaloids and their biological and pharmacological activities. Mar. Drugs 20, 3.  

Ghoran, S. H., Taktaz, F., Ayatollahi, S. A., Kijjoa, A. (2022). Anthraquinones and Their Analogues from Marine‐Derived Fungi: Chemistry and Biological Activities. Mar. Drugs. 20, 474. 

Moreira, J., Silva, P. M. A., Barros, M., Saraiva, L., Pinto, M,. Bousbaa, H., Cidade, H. (2023). Discovery of a New Chalcone-Trimethoxycinnamide Hybrid with Antimitotic Effect: Design, Synthesis, and Structure—Activity Relationship Studies, Pharmaceuticals, 16, 879.  

Almeida, M. C., Szemerédi, N., Durães, F., Long, S., Resende, D. I. S. P., Costa, P. M., Pinto, M., Spengler, G.,  Sousa, E. (2023). Effect of Indole-Containing Pyrazino[2,1-b]quinazoline-3,6-diones in the Virulence of Resistant Bacteria, Antibiotics, 12, 922.   

Soares, J. X., Afonso, I., Omerbasic, A., Loureiro, D. R. P., Pinto, M. M. M., Afonso, C. M. M. (2023).  The Chemical Space of Marine Antibacterials: Diphenyl Ethers, Benzophenones, Xanthones, and Anthraquinones. Molecules, 28, 4073.   

Vilas‑Boas, C., Silva, E. R., Resende, D., Pereira, B., Sousa, G., Pinto, M., Almeida, J. R., Correia‑da‑Silva, M., Sousa, E. (2023). 3,4‑Dioxygenated xanthones as antifouling additives for marine coatings: in silico studies, seawater solubility, degradability, leaching, and antifouling performance, Environmental Science and Pollution Research, 30, 68987–68997.    

Gonçalves, L., Cravo, S., Fernandes, C., Tiritan, M. E. (2022). Development and evaluation of Pirkle-type chiral stationary phase for flash chromatography, J. Chromatogr. A, 1675. 

Projects