Heterocyclic ketones as inhibitors of histone deacetylase

Anil Vasudevan; Zhiqin Ji; Robin R Frey; Carol K Wada; Douglas Steinman; H Robin Heyman; Yan Guo; Michael L Curtin; Jun Guo; Junling Li; Lori Pease; Keith B Glaser; Patrick A Marcotte; Jennifer J Bouska; Steven K Davidsen; Michael R Michaelides

doi:10.1016/j.bmcl.2003.09.007

Heterocyclic ketones as inhibitors of histone deacetylase

Bioorg Med Chem Lett. 2003 Nov 17;13(22):3909-13. doi: 10.1016/j.bmcl.2003.09.007.

Authors

Anil Vasudevan¹, Zhiqin Ji, Robin R Frey, Carol K Wada, Douglas Steinman, H Robin Heyman, Yan Guo, Michael L Curtin, Jun Guo, Junling Li, Lori Pease, Keith B Glaser, Patrick A Marcotte, Jennifer J Bouska, Steven K Davidsen, Michael R Michaelides

Affiliation

¹ Medicinal Chemistry Technologies, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA. [email protected]

PMID: 14592473
DOI: 10.1016/j.bmcl.2003.09.007

Abstract

Several heterocyclic ketones were investigated as potential inhibitors of histone deacetylase. Nanomolar inhibitors such as 22 and 25 were obtained, the anti-proliferative activity of which were shown to be mediated by HDAC inhibition.

MeSH terms

Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Heterocyclic Compounds / pharmacology*
Histone Deacetylase Inhibitors*
Ketones / chemistry
Ketones / pharmacology*
Kinetics
Structure-Activity Relationship

Substances

Enzyme Inhibitors
Heterocyclic Compounds
Histone Deacetylase Inhibitors
Ketones