UCLA researchers in the Department of Chemistry and Biochemistry have synthesized a series of novel hydroxamic acids and derivatives as selective histone deacetylase (HDAC) inhibitors from simple starting materials.
BACKGROUND:
Histone deacetylase (HDAC) inhibitors are chemical compounds that regulates gene expression by inhibiting histone deacetylases. HDAC inhibitors have a long history of use in psychiatry and neurology as mood stabilizers and anti-epileptics. More recently they are being investigated as possible treatments for cancers, parasitic and inflammatory diseases. HDAC inhibition has been for over a decade, and continues to remain, a highly competitive area of drug development. Hydroxamic acids represent the largest class of HDAC inhibitors.
INNOVATION:
UCLA researchers in the Department of Chemistry and Biochemistry have synthesized 6 varieties of novel hydroxamic acids and derivatives as selective histone deacetylase (HDAC) inhibitors. The synthesis of the HDAC inhibitors all start with simple and accessible starting materials, and result in candidate chemicals at a high yield of up to 64%. The proposed synthesis routes can be adapted to inspire in synthesis of a host of desired HDAC inhibitors.
POTENTIAL APPLICATIONS:
• Psychiatry: mood stabilizers and anti-depression
• Neurology: anti-epileptics
• Oncology: cancer treatment
• HIV/AIDS treatment
ADVANTAGES:
• Simple starting materials
• High efficiency (overall yield up to 64%)
DEVELOPMENT-TO-DATE:
Chemicals synthesized and characterized.