1373887-67-2Relevant academic research and scientific papers
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
supporting information; experimental part, 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.
