Design and synthesis of novel 3, 4-disubstituted pyrazoles for nanomedicine applications against malignant gliomas

MC Franchini, BF Bonini, CM Camaggi, D Gentili…

文献索引：Comes Franchini, Mauro; Bonini, Bianca Flavia; Camaggi, Carlo Maurizio; Gentili, Denis; Pession, Annalisa; Rani, Monica; Strocchi, Elena European Journal of Medicinal Chemistry, 2010 , vol. 45, # 5 p. 2024 - 2033

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被引用次数: 30

摘要

A series of novel 3, 4-disubstituted pyrazoles were synthesized. The cytotoxicity against U87MG glioma cell line have been investigated in vitro and three of these compounds showed promising inhibitory activity on cell growth with an IC50 lower than 90μM. AutoDock molecular docking into type I TGF-β receptor (TGF-β-RI; PDB: 1py5) has been done for lead optimization of the mentioned compounds as potential TGF-β-RI1 inhibitors. In particular, ...