scholarly journals Enantioselective pharmacodynamic and pharmacokinetic analysis of two chiral CNS-active carbamate derivatives of valproic acid

Epilepsia ◽  
2014 ◽  
Vol 55 (12) ◽  
pp. 1944-1952 ◽  
Author(s):  
Tawfeeq Shekh-Ahmad ◽  
Hafiz Mawasi ◽  
John H. McDonough ◽  
Richard H. Finnell ◽  
Bogdan J. Wlodarczyk ◽  
...  
Keyword(s):  
Valproic Acid ◽  
Pharmacokinetic Analysis ◽  
Derivatives Of

Pharmacodynamic and pharmacokinetic analysis of CNS-active constitutional isomers of valnoctamide and sec-butylpropylacetamide — Amide derivatives of valproic acid

2015 ◽  
Vol 46 ◽  
pp. 72-78 ◽  
Author(s):  
Hafiz Mawasi ◽  
Tawfeeq Shekh-Ahmad ◽  
Richard H. Finnell ◽  
Bogdan J. Wlodarczyk ◽  
Meir Bialer
Keyword(s):  
Valproic Acid ◽  
Pharmacokinetic Analysis ◽  
Amide Derivatives ◽  
Derivatives Of

Three Amino Acid Derivatives of Valproic Acid: Design, Synthesis, Theoretical and Experimental Evaluation as Anticancer Agents

2014 ◽  
Vol 14 (7) ◽  
pp. 984-993 ◽  
Author(s):  
Gabriela Luna-Palencia ◽  
Federico Martinez-Ramos ◽  
Ismael Vasquez-Moctezuma ◽  
Manuel Fragoso-Vazquez ◽  
Jessica Mendieta-Wejebe ◽  
...  
Keyword(s):  
Valproic Acid ◽  
Amino Acid ◽  
Anticancer Agents ◽  
Experimental Evaluation ◽  
Amino Acid Derivatives ◽  
Design Synthesis ◽  
Derivatives Of

scholarly journals QSAR, molecular docking, design, and pharmacokinetic analysis of 2-(4-fluorophenyl) imidazol-5-ones as anti-breast cancer drug compounds against MCF-7 cell line

2020 ◽  
Vol 52 (6) ◽  
pp. 475-494
Author(s):  
Hadiza Abdulrahman Lawal ◽  
Adamu Uzairu ◽  
Sani Uba
Keyword(s):  
Breast Cancer ◽  
Molecular Docking ◽  
Cell Line ◽  
Docking Studies ◽  
Cancer Drug ◽  
Pharmacokinetic Analysis ◽  
Analysis Model ◽  
Molecular Docking Studies ◽  
Derivatives Of ◽  
Mcf 7

AbstractThe anti-proliferative activities of Novel series of 2-(4-fluorophenyl) imidazol-5-ones against MCF-7 breast cancer cell line were explored via in-slico studies which includes Quantitative structure–activity relationship QSAR, molecular docking studies, designing new compounds, and analyzing the pharmacokinetics properties of the designed compounds. From the QSAR analysis, model number one emerged the best as seen from the arithmetic assessments of (R2) = 0.6981, (R2adj) = 0.6433, (Q2) = 0.5460 and (R2pred) of 0.5357. Model number one was used in designing new derivative compounds, with higher effectiveness against estrogen positive breast cancer (MCF-7 cell line). The Molecular docking studies between the derivatives and Polo-like kinases (Plk1) receptor proved that the derivatives of 2-(4-fluorophenyl) imidazol-5-ones bind tightly to the receptor, thou ligand 24 and 27 had the highest binding affinities of −8.8 and − 9.1 kcal/mol, which was found to be higher than Doxorubicin with a docking score of −8.0 kcal/mol. These new derivatives of 2-(4-fluorophenyl) imidazol-5-ones shall be excellent inhibitors against (plk1). The pharmacokinetics analysis performed on the new structures revealed that all the structures passed the test and also the Lipinski rule of five, and they could further proceed to pre-clinical tests. They both revealed a revolution in medicine for developing novel anti-breast cancer drugs against MCF-7 cell line.

Pharmacokinetic analysis and anticonvulsant activity of two polyesteric prodrugs of valproic acid

1993 ◽  
Vol 14 (1) ◽  
pp. 51-59 ◽  
Author(s):  
Salim Hadad ◽  
Tom B. Vree ◽  
Eppo Van Der Kleijn ◽  
Meir Bialer
Keyword(s):  
Valproic Acid ◽  
Anticonvulsant Activity ◽  
Pharmacokinetic Analysis

Teratology study of derivatives of tetramethylcyclopropyl amide analogues of valproic acid in mice

2006 ◽  
Vol 77 (3) ◽  
pp. 227-233 ◽  
Author(s):  
Akinobu Okada ◽  
Yuko Onishi ◽  
Yoshinobu Aoki ◽  
Boris Yagen ◽  
Eyal Sobol ◽  
...  
Keyword(s):  
Valproic Acid ◽  
Derivatives Of

Organosulfur derivatives of the HDAC inhibitor valproic acid sensitize human lung cancer cell lines to apoptosis and to cisplatin cytotoxicity

2012 ◽  
Vol 227 (10) ◽  
pp. 3389-3396 ◽  
Author(s):  
Anna Tesei ◽  
Giovanni Brigliadori ◽  
Silvia Carloni ◽  
Francesco Fabbri ◽  
Paola Ulivi ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Valproic Acid ◽  
Cell Lines ◽  
Cancer Cell ◽  
Hdac Inhibitor ◽  
Human Lung ◽  
Human Lung Cancer ◽  
Lung Cancer Cell ◽  
Human Lung Cancer Cell ◽  
Derivatives Of

scholarly journals Stereoselective anticonvulsant and pharmacokinetic analysis of valnoctamide, a CNS-active derivative of valproic acid with low teratogenic potential

Epilepsia ◽  
2013 ◽  
Vol 55 (2) ◽  
pp. 353-361 ◽  
Author(s):  
Tawfeeq Shekh-Ahmad ◽  
Naama Hen ◽  
Boris Yagen ◽  
John H. McDonough ◽  
Richard H. Finnell ◽  
...  
Keyword(s):  
Valproic Acid ◽  
Pharmacokinetic Analysis ◽  
Active Derivative ◽  
Teratogenic Potential
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