2400-97-7Relevant articles and documents
Solid-phase combinatorial synthesis and cytotoxicity of 3-aryl-2,4-quinazolindiones
Park Choo, Hea-Young,Kim, Mihyun,Lee, Sang Kook,Woong Kim, Sang,Kwon Chung, In
, p. 517 - 523 (2002)
A series of 3-aryl-2,4-quinazolinediones with various substitution on aromatic rings has been prepared by solid-phase synthesis. Several compounds showed cytotoxicity on human colon carcinoma (Col2) tested by SRB method.
Oxidative Rearrangement of Isatins with Arylamines Using H2O2 as Oxidant: A Facile Synthesis of Quinazoline-2,4-diones and Evaluation of Their Antibacterial Activity
Shi, Guanghao,He, Xinwei,Shang, Yongjia,Yang, Cheng,Xiang, Liwei
, p. 1835 - 1843 (2017/09/06)
A green and highly efficient synthetic method for the synthesis of quinazoline-2,4-diones with hydrogen peroxide as the terminal oxidant has been developed. The reaction features the mild reaction conditions, broad substrate scope, metal-free catalysts, and sole byproduct water. A plausible mechanism for this process was proposed. Moreover, an antibacterial activity study was performed to evaluate the antimicrobial activities towards two Gram-negative bacterial strains (Escherichia coli, and Klebsiella pneumonia) and two Gram-positive bacterial strains (Staphylococcus epidermidis, and Staphylococcus aureus) using the Broth microdilution method.
Molecular modeling studies and synthesis of novel methyl 2-(2-(4-Oxo-3-aryl-3,4-dihydroquinazolin-2-ylthio)acetamido)alkanoates with potential anti-cancer activity as inhibitors for methionine synthase
Elfekki, Ismail Mahmoud,Hassan, Walid Fathalla Mohamed,Elshihawy, Hosam Eldin Abd Elhamed,Ali, Ibrahim Ahmed Ibrahim,Eltamany, Elsayed Hussein Mostafa
, p. 675 - 694 (2014/08/05)
Cobalamin-dependant cytosolic enzyme methionine synthase (MetS) catalyses the transfer of a methyl group from the methyltetrahydrofolate (MTHF) to homocysteine (Hcy) to produce methionine and tetrahydrofolate (THF). MetS is over-expressed in the cytosol of certain breast and prostate tumour cells. Methionine used as a source of one carbon atom for the building of the DNA of the tumour cells, structural protein and enzymes. In this study, we designed, synthesized and evaluated the cytotoxic activity of a series of substituted methyl 2-(2-(4-oxo-3-aryl-3,4-dihydroquinazolin-2-ylthio)acetamido)acetate and dipeptide that mimic the substructure of MTHF. These inhibitors were docked in to the MTHF binding domain in such the same way as MTHF in its binding domain. The free energies of the binding were calculated and compared to the IC 50 values. This series has been developed by dicyclohexylcarbodiimide (DCC) and azide coupling methods of amino acid esters with carboxylic acid derivatives, respectively. Compound methyl 3-hydroxy-2-(2-(3-(4-methoxyphenyl)- 4-oxo-3,4-dihydroquinazolin-2-ylthio)acetamido)propanoate exhibited the highest IC50 value 20 μg/mL against PC-3 cell line and scored the lowest free energy of the binding (-07.19 kJ/mol).
