Spiro[chromane-2,4′-piperidine]-Based Histone Deacetylase Inhibitors with Improved in vivo Activity (pages 709–721)
Dr. Florian Thaler, Dr. Mario Varasi, Dr. Giacomo Carenzi, Dr. Andrea Colombo, Dr. Agnese Abate, Dr. Chiara Bigogno, Dr. Roberto Boggio, Dr. Simone Carrara, Dr. Tiziana Cataudella, Dr. Roberto Dal Zuffo, Dr. Veronica Reali, Dr. Stefania Vultaggio, Dr. Giulio Dondio, Dr. Stefania Gagliardi, Prof. Dr. Saverio Minucci and Ciro Mercurio
Version of Record online: 22 FEB 2012 | DOI: 10.1002/cmdc.201200024
Spiraling to new heights in HDAC inhibition: Herein we summarize the synthesis and biological evaluation of a series of spirochromane hydroxamic acid derivatives as novel inhibitors of human histone deacetylases. Selected compounds were studied for their in vivo pharmacokinetic behavior and for their antitumor activity in an HCT-116 xenograft model.