Synthesis and functionalization of a lactam-pyrazole molecular scaffold as a promising anticancer compound

Bertuzzi, Giulio (2015) Synthesis and functionalization of a lactam-pyrazole molecular scaffold as a promising anticancer compound. [Laurea magistrale], Università di Bologna, Corso di Studio in Chimica industriale [LM-DM270], Documento ad accesso riservato.
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Abstract

The importance of pyrazole and lactam-based molecules in medical and pharmaceutical fields is underlined by the multitude of active ingredients on trade, such as Sildenafil or Apixaban, by Pfizer. In this work, a synthesis of an organic molecule with promising anticancer activity has been developed. This molecular scaffold is characterized by a δ-lactam-fused pyrazolic core, with a well-known biological activity and amenable of further functionalization. The synthetic strategy adopted for the obtainment of the core was based on a 1,3-dipolar cycloaddition of a nitrilimine with an α,β-unsaturated δ-lactam. Secondly, in order to give the final compound an elevated pharmacological activity, a functionalization with a double “side chain”, namely molecular fragment able to improve the interaction with particular biological receptors, was achieved. The target compound was thus obtained, with a highly convergent synthesis, and will be tested for antiproliferative activities towards different cellular lines.

Abstract
Tipologia del documento
Tesi di laurea (Laurea magistrale)
Autore della tesi
Bertuzzi, Giulio
Relatore della tesi
Correlatore della tesi
Scuola
Corso di studio
Parole chiave
pyrazole lactam 1,3-dipolar cycloaddition medicinal chemistry
Data di discussione della Tesi
24 Luglio 2015
URI

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