Abstract

A new tridentate 2-phenyl-imidazopyridin-dipropylacetamide ligand (CB239-H) with high (nanomolar) affinity for the TSPO protein was synthesized and its coordination compound with rhenium tricarbonyl, fac-[Re(CO)3(CB239-N,N,O)] was investigated. The procedure established for the synthesis of the 187/185Re complex can be also used for the synthesis of 99mTc and 188/186Re analogues, which find application in SPECT diagnosis and in therapy. Because of the tridentate coordination of CB239-H and the kinetic inertness of the carbonyl ligands, the new complex was expected to exhibit low reactivity towards plasma proteins and hence greater resistance to deactivation. Being TSPO overexpressed in numerous types of cancers and in activated microglial cells occurring in inflammatory neurodegenerative diseases, TSPO ligands can be exploited as carriers for receptor-mediated drug targeting and hence can be used in diagnosis as well as in therapy. Very suprisingly, fac-[Re(CO)3(CB239-N,N,O)] resulted to be not very stable in diluted human serum but maintained a good affinity towards TSPO.

Autore Pugliese

• Margiotta Nicola , Denora Nunzio , Laquintana Valentino

Tutti gli autori

• NATILE G.;TRAPANI G.;MARGIOTTA N.;DENORA N.;LAQUINTANA V.

Titolo volume/Rivista

Non Disponibile

Anno di pubblicazione

2013

ISSN

1521-3749

ISBN

Non Disponibile

Numero di citazioni Wos

8

Ultimo Aggiornamento Citazioni

Non Disponibile

Numero di citazioni Scopus

10

Ultimo Aggiornamento Citazioni

Non Disponibile

Settori ERC

Non Disponibile

Codici ASJC

Non Disponibile