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Synthesis, in silico and in vitro anti-proliferative studies of some novel benzamido substituted imidazo[1,2-b]pyridazin-2-ones
2017
Journal:  
Ankara Üniversitesi Eczacılık Fakültesi Dergisi
Author:  
Abstract:

ted for their possible anti-proliferative activity. The title compounds were accomplished by the reaction of various 4-Arylidine-2-Phenyl-Oxazol-5-Ones with 3-Aminopyridazine in the presence of ethylene glycol. The chemical structures of the synthesized compounds was characterised by IR, 1H NMR, 13C NMR, Mass spectra and elemental analysis. The synthesized compounds were evaluated for their possible anti-proliferative activity on human cancer cell lines A375 and Colo-205 using MTT assay. Among the tested compounds, compound 6m and 6n showed potent anti-proliferative activity on both cell lines and compounds 6i, 6g and 6d also demonstrated significant activity. Molecular properties and toxicity were predicted for compounds 6a-6n with OSIRIS property explorer. All the tested compounds were proved to be druggable candidates and free from toxicity and teratogenecity. The molecular docking studies of synthesized compounds 6a-6n on B-Raf V600E kinase (PDB ID: 3IDP) further revealed that the active compounds bound to the active site and interacting with Cys532, Phe595, Lys483 residues are comparable with the interactions of Dabrafenib. These studies broadened the scope of imidazo[1,2-b]pyridazine benzamides as promising antiproliferative agents.

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Ankara Üniversitesi Eczacılık Fakültesi Dergisi

Field :   Sağlık Bilimleri

Journal Type :   Uluslararası

Metrics
Article : 863
Cite : 479
2023 Impact : 0.032
Ankara Üniversitesi Eczacılık Fakültesi Dergisi