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Exploiting the 4-Phenylquinazoline Scaffold for the Development of High Affinity Fluorescent Probes for the Translocator Protein (TSPO).

Abstract：

:The quinazoline class was exploited to search for a new translocator protein (TSPO) fluorescent probe endowed with improved affinity and residence time (RT). Computational studies on an "in-house" collection of quinazoline derivatives, featuring highly steric demanding groups at the amide nitrogen, suggested that, despite their molecular extension, these ligands are still easily lodged in the TSPO binding site. Binding assays supported this hypothesis, highlighting a low nanomolar/subnanomolar affinity of these ligands, together with a higher RT of the representative compound 11 with respect to our previously reported indole-based fluorescent probe. Thanks to the amenability of the amide nitrogen atom to be substituted with bulky groups, we developed quinazoline-based imaging tools by fluorescently labeling the scaffold at this position. Probes with relevant TSPO affinity, favorable spectroscopic properties, and improved RT were identified. The results from fluorescence microscopy showed that these probes specifically labeled the TSPO at the mitochondrial level in the U343 cell line.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Milite C,Barresi E,Da Pozzo E,Costa B,Viviano M,Porta A,Messere A,Sbardella G,Da Settimo F,Novellino E,Cosconati S,Castellano S,Taliani S,Martini C

doi

10.1021/acs.jmedchem.7b01031

subject

Has Abstract

pub_date

2017-09-28 00:00:00

pages

7897-7909

issue

18

eissn

0022-2623

issn

1520-4804

journal_volume

60

pub_type

杂志文章

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