Giuseppe Campiani is full professor of Medicinal Chemistry at the University of Siena-IT, Department of Biotechnology, Chemistry and Pharmacy and Adjunct Faculty Member at Isfahan University of Medical Sciences - Isfahan. He started his career as a senior researcher in MedChem working at Siena University and in the early ‘90s, he moved at Mayo Clinic Jacksonville-FL collaborating with Prof. Alan P Kozikowski and later he continued his research activity at Columbia University in the City of New York-Department of Chemistry, as a visiting scientist collaborating with Prof. Koji Nakanishi. In 2001 he was visiting professor at Trinity College Dublin-IRL. Exploration of chemistry and biology of naturally-occurring and synthetic organic molecules with therapeutic potential in infectious diseases, rare diseases and cancer are among of the main topic of his research activity. These interests include target selection and the rational design of innovative drugs, the discovery of new synthetic methodologies and general strategies for synthesis, bioinformatics and the study of important structure-function relationships.