Design, synthesis, and biological evaluation of a new series of pyrazole derivatives: Discovery of potent and selective JNK3 kinase inhibitors

Compound 1f JNK3 kinase, IC50 = 97.4 nM (selective) Sub-micromolar IC50 values against nine cancer cell lines WI-38 normal cells, IC50 = 16.84 µM (high selectivity indexes) Inducer of apoptosis and necrosis in RPMI-8226 leukemia cells NanoBRET assay, IC50 = 3.84 µM Weak inhibitor of CYP 2D6, CYP 3A4...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2022-09, Vol.69, p.116894-116894, Article 116894
Hauptverfasser:	Abu Rabah, Reinad R., Sebastian, Anusha, Vunnam, Srinivasulu, Sultan, Shaista, Tarazi, Hamadeh, Anbar, Hanan S., Shehata, Mahmoud K., Zaraei, Seyed-Omar, Elgendy, Sara M., Al Shamma, Salma A., Omar, Hany A., Al-Tel, Taleb H., El-Gamal, Mohammed I.
Format:	Artikel
Sprache:	eng
Schlagworte:	Cancer JNK3 kinase Kinase inhibitors Molecular modeling Pyrazole Urea
Online-Zugang:	Volltext
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