1373887-64-9Relevant academic research and scientific papers
Exploiting the 4-Phenylquinazoline Scaffold for the Development of High Affinity Fluorescent Probes for the Translocator Protein (TSPO)
Milite, Ciro,Barresi, Elisabetta,Da Pozzo, Eleonora,Costa, Barbara,Viviano, Monica,Porta, Amalia,Messere, Anna,Sbardella, Gianluca,Da Settimo, Federico,Novellino, Ettore,Cosconati, Sandro,Castellano, Sabrina,Taliani, Sabrina,Martini, Claudia
, p. 7897 - 7909 (2017/10/06)
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 st
Structure-activity relationship refinement and further assessment of 4-phenylquinazoline-2-carboxamide translocator protein ligands as antiproliferative agents in human glioblastoma tumors
Castellano, Sabrina,Taliani, Sabrina,Viviano, Monica,Milite, Ciro,Da Pozzo, Eleonora,Costa, Barbara,Barresi, Elisabetta,Bruno, Agostino,Cosconati, Sandro,Marinelli, Luciana,Greco, Giovanni,Novellino, Ettore,Sbardella, Gianluca,Da Settimo, Federico,Martini, Claudia
, p. 2413 - 2428 (2014/04/17)
Structure-activity relationships (SARs) within the 4-phenylquinazoline-2- carboxamide series of translocator protein (TSPO) ligands have been explored further by the synthesis and TSPO binding affinity evaluation of N-benzyl-N-ethyl/methyl derivatives var
Synthesis and biological evaluation of 4-phenylquinazoline-2-carboxamides designed as a novel class of potent ligands of the translocator protein
Castellano, Sabrina,Taliani, Sabrina,Milite, Ciro,Pugliesi, Isabella,Da Pozzo, Eleonora,Rizzetto, Elisa,Bendinelli, Sara,Costa, Barbara,Cosconati, Sandro,Greco, Giovanni,Novellino, Ettore,Sbardella, Gianluca,Stefancich, Giorgio,Martini, Claudia,Da Settimo, Federico
, p. 4506 - 4510 (2012/09/08)
A series of novel 4-phenylquinazoline-2-carboxamides (1-58) were designed as aza-isosters of PK11195, the well-known 18 kDa translocator protein (TSPO) reference ligand, and synthesized by means of a very simple and efficient procedure. A number of these derivatives bind to the TSPO with Ki values in the nanomolar/subnanomolar range, show selectivity toward the central benzodiazepine receptor (BzR) and exhibit structure-affinity relationships consistent with a previously published pharmacophore/topological model of ligand-TSPO interaction.
