کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1373233 | 981893 | 2007 | 5 صفحه PDF | دانلود رایگان |
Novel δ-lactam-based HDAC inhibitors which have various substituted benzyl, bi-aromatic cap groups were prepared using ring closure metathesis reaction, and evaluated their HDAC inhibitory activities and anti-proliferative effects. Among prepared analogues, 11m and 11o have very strong HDAC enzymatic inhibition and showed the most potent growth inhibitory activity to five human tumor cell lines including PC-3, ACHN, NUGC-3, HCT-15, and MBA-MB-231 tumor cell lines. Compounds 11m and 11o also showed good tumor growth inhibition of MDA-MB-231 cells in in vivo xenograft model. Structure–activity relationship study using docking model explained the significance of hydrophobic aromatic cap groups for their in vitro activities.
Novel δ-lactam-based HDAC inhibitors with various substituted benzyl or bi-aromatic CAP groups were prepared using ring closure metathesis reaction, and their HDAC inhibitory activities and anti-proliferative effects evaluated.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 22, 15 November 2007, Pages 6234–6238