Abstract
HDAC inhibitors show great promise for the treatment of cancer. As part of a broader effort to explore the SAR of HDAC inhibitors, synthesis, biological evaluation, and molecular docking of novel Ugi products containing a zinc-chelating moiety are presented. One compound shows improved inhibitory potencies compared to SAHA, demonstrating that hindered lipophilic residues grafted on the peptide scaffold of the α-aminoacylamides can be favorable in the interaction with the enzyme.
Original language | English |
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Pages (from-to) | 2776-2785 |
Number of pages | 10 |
Journal | Journal of Medicinal Chemistry |
Volume | 52 |
Issue number | 9 |
DOIs | |
Publication status | Published - 14 May 2009 |