Pelliccia, Sveva (2013) Drug design, chemical optimization and biological evaluation of pre-existing scaffolds towards selected therapeutic targets. [Tesi di dottorato]
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| Tipologia del documento: | Tesi di dottorato |
|---|---|
| Lingua: | English |
| Titolo: | Drug design, chemical optimization and biological evaluation of pre-existing scaffolds towards selected therapeutic targets. |
| Autori: | Autore Email Pelliccia, Sveva sveva.pelliccia@unina.it |
| Data: | 30 Marzo 2013 |
| Numero di pagine: | 231 |
| Istituzione: | Università degli Studi di Napoli Federico II |
| Dipartimento: | Farmacia |
| Scuola di dottorato: | Scienze farmaceutiche |
| Dottorato: | Scienza del farmaco |
| Ciclo di dottorato: | 25 |
| Coordinatore del Corso di dottorato: | nome email D'Auria, Maria Valeria madauria@unina.it |
| Tutor: | nome email Grieco, Paolo pagrieco@unina.it |
| Data: | 30 Marzo 2013 |
| Numero di pagine: | 231 |
| Parole chiave: | Urotensin-II, Tubulin, GSK-3beta |
| Settori scientifico-disciplinari del MIUR: | Area 03 - Scienze chimiche > CHIM/08 - Chimica farmaceutica |
| Depositato il: | 09 Apr 2013 11:45 |
| Ultima modifica: | 10 Giu 2015 12:43 |
| URI: | http://www.fedoa.unina.it/id/eprint/9213 |
Abstract
In this PhD thesis, I have focused my attention on drug design, chemical optimization and biological evaluation of pre-existing scaffolds towards selected therapeutic targets, such as UT-II receptor, tubulin and GSK-3beta. Firstly, I reported the synthesis of potential agonists and antagonists of UT-II receptor. These compounds share a monoketopiperazine scaffold, decorated with appropriate aminoacid residues that are pharmacophoric for UTR-II. Secondly, I presented the results about new 2-heterocyclyl-3-arylthio-1H-indoles as anticancer agents. Some derivatives exhibited potent tubulin assembly and cancer cell growth inhibition in vitro and in vivo assays. Thirdly, I showed the synthesis of new GSK-3beta inhibitors as potential anti-Alzheimer agents. New derivatives were obtained by chemical modification of a recently identified hit compound, leading to a potent GSK-3beta inhibitory activity in the low micromolar range of concentration.
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