Fluorine in bioorganic chemistry


Fiorenza Viani, Fiorenza.viani@polimi.it1, Matteo Zanda, matteo.zanda@polimi.it1, Alessandro Volonterio, alessandro.volonterio@polimi.it2, Cristina Pesenti2, Monica Sani2, and Roberta Sinisi2. (1) Istituto di Chimica del Riconoscimento Molecolare, Consiglio Nazionale delle Ricerche, Via Mancinelli 7, 20131 Milano, Italy, (2) Dipartimento di Chimica, Materiali e Ingegneria Chimica "G. Natta", Politecnico di Milano, via Mancinelli 7, I-20131 Milan, Italy
The incorporation of fluorine into organic molecules can be an effective strategy for improving and modifying the biological activity. Actually, the introduction of fluorine into key-positions of drug like molecules can be an effective way for optimizing and tuning their biological and/or pharmacological properties. Particular emphasis will be given to the effects of the introduction of a trifluoromethyl group that is recognized in medicinal chemistry as a substituent of distinctive qualities. In particular, its incorporation into some families of pharmacologically active agents, such as proteinase inhibitors having or not peptidomimetic structures and displaying anti-cancer, anti-HIV and anti-malaric activity could be a strategy for modifying the binding properties and the selectivity towards the targeted enzymes. Biological results and crystal structure analyses will help to verify the hypothesis.