Design of small molecule inhibitors of human voltage gated sodium channels for treatment of prostate cancer

ORGN 324

Gary Davis, garycdavis@gmail.com, Thomas Walls, thw4g@virginia.edu, Simeng Suy, suys@georgetown.edu, Li Zhang, Milton L. Brown, mb544@georgetown.edu, and Sivanesan Dakshanamurthy, sd233@georgetown.edu. Drug Discovery Program, Georgetown University Medical Center, 3970 Reservoir Road, Washington, DC 20057
α-Hydroxy-α-phenylamides are a new class of chiral small molecules that have demonstrated potent inhibition of human voltage-gated sodium channels. In this talk we will discuss the use of Seebach and Frater's chiral template and other methodologies to obtain each pure enantiomer of the lead compound. Finally we evaluated these compounds for functional blockade of human sodium channels and measured their effects on human prostate cancer cell proliferation and in vivo activity on the growth of human prostate tumor xenografts.
 

Small Molecule Therapeutic Agents
8:30 AM-11:50 AM, Tuesday, August 18, 2009 Walter E. Washington Convention Center -- 207A, Oral

Division of Organic Chemistry

The 238th ACS National Meeting, Washington, DC, August 16-20, 2009