Medicinal Chemistry - Synthesis of biologically active small molecules. Coordinator: Minarini

Design and synthesis of small molecules as potential drugs and/or pharmacological tools for the study of biological pathways in the context of chronic-degenerative diseases, such as Alzheimer's disease and cancer

Research themes

The research activity of the group focuses on the design and synthesis of multifunctional ligands as modulators of targets and biological pathways involved in neurodegeneration and cancer. In particular, the research lines cover the development of:
• antioxidant molecules
• Aβ peptide antiaggregating molecules

• acetylcholinesterase inhibitors
• topoisomerase inhibitors and DNA intercalators
• amino oxidase inhibitors
The group has a documented expertise in the structural modification of natural compounds, quinazoline derivatives and aromatic heterocycles, and in the synthesis of polyamine conjugated of bioactive molecules to improve the cellular and subcellular cellular delivery.

Lab members

Prof. Anna Minarini (write), visit her institutional website

Prof. Michela Rosini (write), visit her institutional website

Dr. Filippo Basagni (write)

Dr. Giambattista Marotta (write)

Internship projects

Every year the research group can guest 4 students for the preparation of the experimental thesis that takes place in about 8 months and, every three years, a position for the PhD program. The thesis work consists in the synthesis, purification and characterization of organic molecules designed on the basis of ongoing research projects in the group.

Main publications

Basagni F, Lanni C, Minarini A, Rosini M. Lights and shadows of electrophile signaling: focus on the Nrf2-Keap1 pathway. Future Med, Chem., 2019, 11, 707-721. 10.4155/fmc-2018-0423

Simoni E, Serafini MM, Caporaso R, Marchetti C, Racchi M, Minarini A, Bartolini B, Lanni C, Rosini M. Targeting the Nrf2/Amyloid-Beta Liaison in Alzheimer's Disease: A Rational Approach. ACS Chem. Neurosci., 2017, 8, 1618-1627. 10.1021/acschemneuro.7b00100

Simoni E, Caporaso R, Bergamini C, Fiori J, Fato R, Miszta P, Filipek S, Caraci F, Giuffrida ML, Andrisano V, Minarini A, Bartolini B, Rosini M. Polyamine Conjugation as a Promising Strategy To Target Amyloid Aggregation in the Framework of Alzheimer’s Disease. ACS Med. Chem. Lett., 2016, 7, 1145–1150. 10.1021/acsmedchemlett.6b00339

Palermo G, Minniti E, Greco ML, Riccardi L, Simoni E, Convertino M, Marchetti C, Rosini M, Sissi C, Minarini A, De Vivo M. An optimized polyamine moiety boosts the potency of human type II topoisomerase poisons as quantified by comparative analysis centered on the clinical candidate F14512. Chem. Commun., 2015, 51, 14310-14313. 2015/cc/c5cc05065k

Rosini M, Simoni E, Milelli A, Minarini A, Melchiorre C. Oxidative stress in Alzheimer’s disease: are we connecting the dots? J. Med. Chem. 2014, 57, 2821-2831. 10.1021/jm400970m