Pyrrole‐Based Hydroxamates and 2‐Aminoanilides: Histone Deacetylase Inhibition and Cellular Activities

Abstract

Pyrrole-based HDAC inhibitors: Pyrrolyl-hydroxamates (3 a–g) and 2-aminoanilides (4 a–g) derived from the class II-selective histone deacetylase (HDAC) inhibitor MC1568 (1) were prepared and tested against human recombinant HDAC1, HDAC4, and HDAC6. Unlike compound 1, most of the tested compounds inhibited both HDAC1 and HDAC6, and were less potent or completely inactive against HDAC4. Consistent with their high HDAC1/HDAC6 inhibition, compounds 3 a and 3 b induced>20 % cell death in U937 cells at 1 μm. Detailed facts of importance to specialist readers are published as ”Supporting Information”. Such documents are peer-reviewed, but not copy-edited or typeset. They are made available as submitted by the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.