A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units

Yujia Dai; Yan Guo; Michael L Curtin; Junling Li; Lori J Pease; Jun Guo; Patrick A Marcotte; Keith B Glaser; Steven K Davidsen; Michael R Michaelides

doi:10.1016/j.bmcl.2003.07.012

A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units

Bioorg Med Chem Lett. 2003 Nov 3;13(21):3817-20. doi: 10.1016/j.bmcl.2003.07.012.

Authors

Yujia Dai¹, Yan Guo, Michael L Curtin, Junling Li, Lori J Pease, Jun Guo, Patrick A Marcotte, Keith B Glaser, Steven K Davidsen, Michael R Michaelides

Affiliation

¹ Cancer Research, Abbott Laboratories, Department R47J, Building AP10, 100 Abbott Park Road, Abbott Park, IL 60031, USA. yujia.dai@abbott.com

PMID: 14552787
DOI: 10.1016/j.bmcl.2003.07.012

Abstract

A series of structurally novel HDAC inhibitors, in which a hetero aromatic ring connects the spacer with the hydrophobic group, has been designed and synthesized. These new inhibitors are very potent in in vitro enzymatic assays and display antiproliferation activity against two human cancer cell lines.

MeSH terms

Cell Division / drug effects
Cell Line, Tumor
Chemical Phenomena
Chemistry, Physical
Crystallography, X-Ray
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology*
Histone Deacetylase Inhibitors*
Humans
Hydroxamic Acids / antagonists & inhibitors
Hydroxamic Acids / pharmacology
Indicators and Reagents
Structure-Activity Relationship

Substances

Enzyme Inhibitors
Histone Deacetylase Inhibitors
Hydroxamic Acids
Indicators and Reagents