CoMFA, Synthesis, and Pharmacological Evaluation of (E)-3-(2-Carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic Acids:  3-[2-(3-Aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic Acid, a Potent Selective Glycine-Site NMDA Receptor Antagonist†

2005 ◽  
Vol 48 (4) ◽  
pp. 995-1018 ◽  
Author(s):  
Bruce M. Baron ◽  
Robert J. Cregge ◽  
Robert A. Farr ◽  
Dirk Friedrich ◽  
Raymond S. Gross ◽  
...  
Keyword(s):  
Nmda Receptor ◽  
Carboxylic Acid ◽  
Receptor Antagonist ◽  
Carboxylic Acids ◽  
Nmda Receptor Antagonist ◽  
Glycine Site ◽  
Pharmacological Evaluation

scholarly journals Synthesis and Cytotoxic Activity Evaluation of New Cu(I) Complexes of Bis(pyrazol-1-yl) Acetate Ligands Functionalized with an NMDA Receptor Antagonist

2020 ◽  
Vol 21 (7) ◽  
pp. 2616 ◽  
Author(s):  
Maura Pellei ◽  
Luca Bagnarelli ◽  
Lorenzo Luciani ◽  
Fabio Del Bello ◽  
Gianfabio Giorgioni ◽  
...  
Keyword(s):  
Nmda Receptor ◽  
Carboxylic Acid ◽  
Receptor Antagonist ◽  
Three Dimensional ◽  
Human Tumor ◽  
Nmda Antagonist ◽  
Nmda Receptor Antagonist ◽  
Ic50 Values ◽  
Drug Resistant Phenotype

In the present article, copper(I) complexes of bis(pyrazol-1-yl) carboxylic acid (LH), bis(3,5-dimethylpyrazol-1-yl) carboxylic acid (L2H), and bis(pyrazol-1-yl) acetates conjugated with an N-methyl-d-aspartate (NMDA) receptor antagonist (LNMDA or L2NMDA) and phosphane ligands (triphenylphosphine or 1,3,5-triaza-7-phosphaadamantane) were synthesized. The selection of an NMDA antagonist for the coupling with LH and L2H was suggested by the observation that NMDA receptors are expressed and play a role in different types of cancer models. All the new complexes showed a significant antitumor activity on a panel of human tumor cell lines of different histology, with cisplatin-sensitive, cisplatin-resistant, or multi-drug-resistant phenotype. Their half maximal inhibitory concentration (IC50) values were in the low- and sub-micromolar range and, in general, significantly lower than that of cisplatin. Interestingly, the fact that all the complexes proved to be significantly more active than cisplatin even in three-dimensional (3D) spheroids of H157 and BxPC3 cancer cells increased the relevance of the in vitro results. Finally, morphological analysis revealed that the most representative complex 8 induced a massive swelling of the endoplasmic reticulum (ER) membrane, which is a clear sign of ER stress.

Chiral synthesis and pharmacological evaluation of NPS 1407: a potent, stereoselective NMDA receptor antagonist

2000 ◽  
Vol 10 (21) ◽  
pp. 2411-2415 ◽  
Author(s):  
Scott T Moe ◽  
Daryl L Smith ◽  
Eric G DelMar ◽  
Scot M Shimizu ◽  
Bradford C Van Wagenen ◽  
...  
Keyword(s):  
Nmda Receptor ◽  
Receptor Antagonist ◽  
Nmda Receptor Antagonist ◽  
Chiral Synthesis ◽  
Pharmacological Evaluation
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