NANOPARTICLES OF A PYRAZOLO-PYRIDAZINE DERIVATIVE AS POTENTIAL EGFR AND CDK-2 INHIBITORS: DESIGN, STRUCTURE DETERMINATION, ANTICANCER EVALUATION AND IN SILICO STUDIES

Nanoparticles of a Pyrazolo-Pyridazine Derivative as Potential EGFR and CDK-2 Inhibitors: Design, Structure Determination, Anticancer Evaluation and In Silico Studies

Nanoparticles of a Pyrazolo-Pyridazine Derivative as Potential EGFR and CDK-2 Inhibitors: Design, Structure Determination, Anticancer Evaluation and In Silico Studies

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The strategic planning of this study is based upon using the nanoformulation method to prepare nanoparticles 4-SLNs and 4-LPHNPs of the previously prepared 4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-3-amine (4) after confirming its structure with single crystal X-ray analysis.These nanoparticles exhibited promising cytotoxic activity against HepG-2, HCT-116 and MCF-7 cancer cell lines Kontekstualisasi Fungsi Bagas Godang dan Sopo Godang Sebagai Sumber Pembelajaran Sejarah Lokal in comparison with the reference doxorubicin and the original derivative 4.Moreover, their inhibitory assessment against EGFR and CDK-2/cyclin A2 displayed improved and more favorable impact than the parent 4 and the references.

Detection of their influence upon cancer biomarkers revealed Text Clustering Algorithm Based on Random Cluster Core upregulation of Bax, p53 and caspase-3 levels and downregulation of Bcl-2 levels.The docking simulation demonstrated that the presence of the pyrazolo[3,4-c]pyridazin-3-amine scaffold is amenable to enclosure and binding well within EGFR and CDK-2 receptors through different hydrophilic interactions.The pharmacokinetic and physicochemical properties of target 4 were also assessed with ADME investigation, and the outcome indicated good drug-like characteristics.

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