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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Item Type:	Tesi di dottorato
Resource language:	English
Title:	Drug design, chemical optimization and biological evaluation of pre-existing scaffolds towards selected therapeutic targets.
Creators:	Creators Email Pelliccia, Sveva sveva.pelliccia@unina.it
Date:	30 March 2013
Number of Pages:	231
Institution:	Università degli Studi di Napoli Federico II
Department:	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
Date:	30 March 2013
Number of Pages:	231
Keywords:	Urotensin-II, Tubulin, GSK-3beta
Settori scientifico-disciplinari del MIUR:	Area 03 - Scienze chimiche > CHIM/08 - Chimica farmaceutica
Date Deposited:	09 Apr 2013 11:45
Last Modified:	10 Jun 2015 12:43
URI:	http://www.fedoa.unina.it/id/eprint/9213

Collection description

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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