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Bioorg Med Chem. 2010 Aug 15;18(16):5950-64. doi: 10.1016/j.bmc.2010.06.081. Epub 2010 Jul 1.

Dual inhibitors of inosine monophosphate dehydrogenase and histone deacetylase based on a cinnamic hydroxamic acid core structure.

Author information

1
Center for Drug Design, Academic Health Center, University of Minnesota, Minneapolis, MN 55455, USA. chenx462@umn.edu

Abstract

Small molecules that act on multiple biological targets have been proposed to combat the drug resistance commonly observed for cancer chemotherapy. By combining the structural features of known inhibitors of inosine monophosphate dehydrogense (IMPDH) and histone deacetylase (HDAC), dual inhibitors of IMPDH and HDAC based on the scaffold of cinnamic hydroxamic acid (CHA) have been designed, synthesized, and evaluated in biological assays. Key features, including the linker length, linker functionality, substitution position, and interacting groups, have been explored. Their individual contribution to the inhibitory activities against human IMPDH1 and IMPDH2 as well as HDAC has been assessed.

PMID:
20650640
DOI:
10.1016/j.bmc.2010.06.081
[Indexed for MEDLINE]

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