Ontology highlight
ABSTRACT:
SUBMITTER: Singh EK
PROVIDER: S-EPMC2593638 | biostudies-literature | 2008 Apr
REPOSITORIES: biostudies-literature
Singh Erinprit K EK Ravula Suchitra S Pan Chung-Mao CM Pan Po-Shen PS Vasko Robert C RC Lapera Stephanie A SA Weerasinghe Sujith V W SV Pflum Mary Kay H MK McAlpine Shelli R SR
Bioorganic & medicinal chemistry letters 20080320 8
We outline the synthesis of six novel derivatives that are based on a recently discovered HDAC inhibitor FR235222. Our work is the first report utilizing a novel binding element, guanidine, as metal coordinators in HDAC inhibitors. Further, we demonstrate that these compounds show cytotoxicity that parallels their ability to inhibit deacetylase activity, and that the most potent compounds maintain an L-Phe at position 1, and a D-Pro at position 4. Both inhibition of HDAC activity and cytotoxicit ...[more]