Pelliccia, Sveva (2013) Drug design, chemical optimization and biological evaluation of pre-existing scaffolds towards selected therapeutic targets. [Tesi di dottorato]

[img] Documento PDF
pelliccia_sveva_25.pdf
Visibile a [TBR] Repository staff only

Download (7MB) | Request a copy
[error in script] [error in script]
Item Type: Tesi di dottorato
Lingua: English
Title: Drug design, chemical optimization and biological evaluation of pre-existing scaffolds towards selected therapeutic targets.
Creators:
CreatorsEmail
Pelliccia, Svevasveva.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:
nomeemail
D'Auria, Maria Valeriamadauria@unina.it
Tutor:
nomeemail
Grieco, Paolopagrieco@unina.it
Date: 30 March 2013
Number of Pages: 231
Uncontrolled 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

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.

Actions (login required)

View Item View Item