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 | ||||
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| Lingua: | English | ||||
| Titolo: | Drug design, chemical optimization and biological evaluation of pre-existing scaffolds towards selected therapeutic targets. | ||||
| Autori: |
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| 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: |
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| Tutor: |
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| 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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