4-Hydroxy-6-Oxo-6,7-Dihydro-Thieno[2,3-b] pyrimidine derivatives: Synthesis and their biological evaluation for the glycine site acting on theN-Methyl-D-aspartate (NMDA) receptor

2001 ◽  
Vol 24 (4) ◽  
pp. 270-275 ◽  
Author(s):  
Ki-Jun Hwang ◽  
Tae-Suk Lee ◽  
Ki-Won Kim ◽  
Beom-Tae Kim ◽  
Chul-Min Lee ◽  
...  
Keyword(s):  
Nmda Receptor ◽  
Biological Evaluation ◽  
Glycine Site ◽  
Pyrimidine Derivatives

GV 196771A, a New Glycine Site Antagonist of the NMDA Receptor with Potent Antihyperalgesic Activity

Pain ◽  
2003 ◽  
Author(s):  
C Carignani ◽  
M Mugnaini ◽  
E Ratti ◽  
M Corsi ◽  
G Dal Forno ◽  
...  
Keyword(s):  
Nmda Receptor ◽  
Glycine Site

ChemInform Abstract: Synthesis, Biological Evaluation and Molecular Docking Studies of Some Pyrimidine Derivatives.

ChemInform ◽  
2013 ◽  
Vol 44 (52) ◽  
pp. no-no
Author(s):  
Ahmed M. Fargualy ◽  
Nargues S. Habib ◽  
Khadiga A. Ismail ◽  
Ahmed M. M. Hassan ◽  
Marwa T. M. Sarg
Keyword(s):  
Molecular Docking ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Pyrimidine Derivatives ◽  
Molecular Docking Studies

Synthesis and Biological Evaluation of Novel 4-Phenylaminobenzofuro[2,3-d]pyrimidine Derivatives

2020 ◽  
Vol 42 (4) ◽  
pp. 564-564
Author(s):  
Ju liu Ju liu ◽  
Jun Li Jun Li ◽  
Jian tao Shi Jian tao Shi ◽  
Jie Li Jie Li ◽  
Xue chen Hao Xue chen Hao ◽  
...  
Keyword(s):  
Cell Lines ◽  
A549 Cells ◽  
Positive Control ◽  
Biological Evaluation ◽  
Dependent Manner ◽  
Pyrimidine Derivatives ◽  
Concentration Dependent Manner ◽  
Ic50 Value ◽  
Synthesis And Biological Evaluation

A series of novel 4-phenylaminobenzofuro[2,3-d]pyrimidine derivatives had been prepared and assessed for their in vitro antiproliferative activities against three lung cancer cell lines (A549, H460 and H1975). The bioassay results showed most of the designed compounds exhibited potential antiproliferation activities. Among them, compound 8f exhibited remarkable inhibitory activity against A549 and H460 cell lines with IC50 value of 2.54 μM and 2.68 μM, respectively, which was comparable to that of the positive control sorafenib (IC50 = 2.69 μM for A549 and 3.71 μM for H460). AO/EB staining suggests that compound 8f could induce apoptosis in A549 cells. Furthermore, cell cycle analyses show that compound 8f increased G0/G1 A549 cells arrest in a concentration-dependent manner. The preliminary structure-activity relationships (SARs) studies indicated that mono-electron-withdrawing groups (mono-EWGs) on the phenyl ring are positive on the antitumor activity.

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