کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1373753 | 981905 | 2009 | 4 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Histone deacetylase inhibitors with a primary amide zinc binding group display antitumor activity in xenograft model Histone deacetylase inhibitors with a primary amide zinc binding group display antitumor activity in xenograft model](/preview/png/1373753.png)
Histone deacetylase (HDAC) inhibition causes hyperacetylation of histones leading to differentiation, growth arrest and apoptosis of malignant cells, representing a new strategy in cancer therapy. Many of the known HDAC inhibitors (HDACi) that are in clinical trials possess a hydroxamic acid, that is a strong Zn2+ binding group, thereby inhibiting some of the class I and class II isoforms. Herein we describe the identification of a selective class I HDAC inhibitor bearing a primary carboxamide moiety as zinc binding group. This HDACi displays good antiproliferative activity against multiple cancer cell lines, and demonstrates efficacy in a xenograft model comparable to vorinostat.
The identification of a selective class I HDAC inhibitor bearing a primary carboxamide as zinc binding group together with its efficacy in vivo is described.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 11, 1 June 2009, Pages 3081–3084