کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1396533 1501189 2010 10 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design and synthesis of novel 3,4-disubstituted pyrazoles for nanomedicine applications against malignant gliomas
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design and synthesis of novel 3,4-disubstituted pyrazoles for nanomedicine applications against malignant gliomas
چکیده انگلیسی

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.

Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 45, Issue 5, May 2010, Pages 2024–2033
نویسندگان
, , , , , , ,