5958-08-7Relevant academic research and scientific papers
4-ARYLQUINAZOLINE DERIVATIVES AS INHIBITORS OF METHIONINE ADENOSYLTRANSFERASE 2A
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, (2021/12/31)
The invention relates to certain derivatives of 4-arylquinazoline formula (I) which are inhibitors of methionine adenosyltransferase 2A (MAT2A). The invention also relates to pharmaceutical compositions comprising such compounds and methods of treating diseases that can be treated by inhibition of MAT2A such as cancer, including cancers characterized by reduced or no activity of methylthioadenosine phosphorylase (MTAP).
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.
Reactions of hydroxyglycines. New synthetic routes to 4-phenylquinazoline derivatives
Hoefnagel,Van Koningsveld,Van Meurs,Peters,Sinnema,Van Bekkum
, p. 6899 - 6912 (2007/10/02)
Reaction of hydroxyglycine with 2-aminobenzophenones gives 1,2-dihydro-4-phenyl-quinazoline-2-carboxylic acids in high yields and under mild conditions. These can be smoothly converted into the corresponding 3,4-dihydro isomers and into quinazoline derivatives via rearrangement and oxidation by air, respectively. The X-ray crystallographic structure of 6-chloro-1,2-dihydro-1-methyl-4-phenylquinazoline-2-carboxylic acid shows the carboxylate group at C(2) and the methyl group at N(1) to be in axial positions.
