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Titolo:
Convergent synthesis of potent peptide inhibitors of the Grb2-SH2 domain by palladium catalyzed coupling of a terminal alkyne
Autore:
Schoepfer, J; Gay, B; End, N; Muller, E; Scheffel, G; Caravatti, G; Furet, P;
Indirizzi:
NOVARTIS Pharma AG, Oncol Res, CH-4002 Basel, Switzerland NOVARTIS Pharma AG Basel Switzerland CH-4002 CH-4002 Basel, Switzerland
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
fascicolo: 9, volume: 11, anno: 2001,
pagine: 1201 - 1203
SICI:
0960-894X(20010507)11:9<1201:CSOPPI>2.0.ZU;2-C
Fonte:
ISI
Lingua:
ENG
Soggetto:
STRUCTURE-BASED DESIGN; SH2 DOMAIN; AFFINITY; LIGANDS; BINDING; THERAPY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
15
Recensione:
Indirizzi per estratti:
Indirizzo: Schoepfer, J NOVARTIS Pharma AG, Oncol Res, CH-4002 Basel, Switzerland NOVARTIS Pharma AG Basel Switzerland CH-4002 l, Switzerland
Citazione:
J. Schoepfer et al., "Convergent synthesis of potent peptide inhibitors of the Grb2-SH2 domain by palladium catalyzed coupling of a terminal alkyne", BIOORG MED, 11(9), 2001, pp. 1201-1203

Abstract

A new strategy was developed to prepare in a very efficient and convergentmanner C-terminal modified tripeptides with high affinities for the Grb2-SH2 domain. Using Pd(PPh3)(2)Cl-2 as catalyst, selected naphthyl iodides andtriflates were coupled to Ac-Pmp(t-Bu)(2)-Ac(6)c-Asn-NH(prop-2-ynyl). The resulting alkyne derivatives were hydrogenated and deprotected to afford potent Grb2-SH2 inhibitors. (C) 2001 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 08/04/20 alle ore 11:48:22