کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1396533 | 1501189 | 2010 | 10 صفحه PDF | دانلود رایگان |

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 90 μM. 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, 3-aryl-4-amido pyrazole containing long ω-amino-aliphatic chain emerged as a good candidate for further optimization. Entrapment into targetable PEG-based micelles improved growth inhibition IC50 values up to 100 nM and this could lead to a novel drug delivery strategy for treating glioblastoma.
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Journal: European Journal of Medicinal Chemistry - Volume 45, Issue 5, May 2010, Pages 2024–2033