1224442-46-9Relevant academic research and scientific papers
Substituted 2-arylquinazolinones: Design, synthesis, and evaluation of cytotoxicity and inhibition of topoisomerases
Khadka, Daulat Bikram,Tran, Giap Huu,Shin, Somin,Nguyen, Hang Thi Minh,Cao, Hue Thi,Zhao, Chao,Jin, Yifeng,Van, Hue Thi My,Chau, Minh Van,Kwon, Youngjoo,Le, Thanh Nguyen,Cho, Won-Jea
, p. 69 - 79 (2015)
A series of 2-arylquinazolinones with structural homology to known 3-arylisoquinolines were designed and synthesized in order to develop safe, effective, and selective cytotoxic agents targeting topoisomerases (topos). 2-Arylquinzolinones with various substitutions on the aromatic rings were obtained by thermal cyclodehydration/dehydrogenation on reacting anthranilamides and benzaldehydes. The compounds had superior topo I-inhibitory activities but were generally inactive against topo IIα. Among the 6-methyl-, 6-amino-, and 7-methylquinazolinones, 6-amino-substituted derivatives displayed potent cytotoxicity at submicromolar to nanomolar concentrations against human colorectal adenocarcinoma cells (HCT-15), human ductal breast epithelial tumor cells (T47D), and cervical cancer cells (HeLa). There was a good correlation between topo I inhibition and the cytotoxic effects of 6-aminoquinazolinones. Docking models demonstrated that topo I inhibition by these compounds is owing to intercalation and H-bond interactions with the DNA bases and amino acid residues at the enzymatic site.
Catalyst/ligand-free synthesis of benzimidazoles and quinazolinones from amidines via intramolecular transamination reaction
Gupta, Sahaj,Agarwal, Piyush K.,Kundu, Bijoy
experimental part, p. 1887 - 1890 (2010/09/07)
An efficient catalyst/ligand-free synthesis of benzimidazoles and quinazolinones from amidines in quantitative yields has been described.
