Design, Synthesis, Photophysical Properties, Biological Estimation and Molecular Docking Studies of Novel Schiff Base Derivatives as Potential Urease Inhibitors

2018 ◽  
Vol 28 (6) ◽  
pp. 1295-1304 ◽  
Author(s):  
Balasaheb D. Vanjare ◽  
Prasad G. Mahajan ◽  
Mubashir Hassan ◽  
Hussain Raza ◽  
Sung-Yum Seo ◽  
...  
Keyword(s):  
Schiff Base ◽  
Molecular Docking ◽  
Photophysical Properties ◽  
Docking Studies ◽  
Urease Inhibitors ◽  
Design Synthesis ◽  
Molecular Docking Studies ◽  
Schiff Base Derivatives

Hydrazine clubbed 1,3-thiazoles as potent urease inhibitors: design, synthesis and molecular docking studies

2020 ◽  
Author(s):  
Pervaiz Ali Channar ◽  
Aamer Saeed ◽  
Saira Afzal ◽  
Dilawar Hussain ◽  
Markus Kalesse ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Docking Studies ◽  
Urease Inhibitors ◽  
Design Synthesis ◽  
Molecular Docking Studies

scholarly journals Chiral Pyridine-3,5-bis- (L-phenylalaninyl-L-leucinyl) Schiff Base Peptides as Potential Anticancer Agents: Design, Synthesis, and Molecular Docking Studies Targeting Lactate Dehydrogenase-A

Molecules ◽  
2020 ◽  
Vol 25 (5) ◽  
pp. 1096
Author(s):  
Abd El-Galil E. Amr ◽  
Randa E. Abdel Mageid ◽  
Mohamed El-Naggar ◽  
Ahmed M. Naglah ◽  
Eman S. Nossier ◽  
...  
Keyword(s):  
Schiff Base ◽  
Molecular Docking ◽  
Lactate Dehydrogenase ◽  
Schiff Bases ◽  
Anticancer Agents ◽  
Docking Studies ◽  
Carcinoma Cells ◽  
Design Synthesis ◽  
Molecular Docking Studies ◽  
Mcf 7

A series of branched tetrapeptide Schiff bases 3–6 were designed and synthesized from corresponding tetrapeptide hydrazide 2 as a starting material.In vitroevaluation of the synthesized compounds 4–6 against breast MCF-7 carcinoma cells identified their excellent anticancer potency, with IC50 ranging from 8.12 ± 0.14 to 17.55 ± 0.27 μM in comparison with the references, cisplatin and milaplatin (IC50= 13.34 ± 0.11and 18.43 ± 0.13 μM, respectively). Furthermore, all derivatives demonstrated promising activity upon evaluation of theirin vitroandin vivosuppression of p53 ubiquitination and inhibition assessment for LDHA kinase. Finally, molecular docking studies were performed to predict the possible binding features of the potent derivatives within the ATP pocket of LDHA in an attempt to get a lead for developing a more potent LDHA inhibitor with anti-proliferative potency.

Sign in / Sign up

Export Citation Format

Share Document