Novel Compounds with Potential Activity for Ovarian Cancer (Case 1992)

Affiliation:

 

Brown University

Providence, RI

 

Brief Description:      

The present invention describes a series of novel compounds, based on the scaffold of N-amino tetrahydrothiazine, that are highly cytotoxic in models for ovarian cancer and other cancers – even exceeding potency of cisplatin, 5-FU, cyclophosphamide and sapacitabine. The mechanism results from a reduction in mitochondrial transmembrane depolarization potential. Even at sub-toxic doses, the lead compound, RKS262, delays cell cycle progression through the G2 phase and up-regulates p27 while cyclin D1 and Cdk-6 are down-regulated, including that RKS262 is a specific cyclin/CDK inhibitor. The compound is expected to be able to cross the blood-brain barrier. Studies in the xenograft rodent model show a significant dose-dependent decrease in tumor growth in animals provided with RKS262.

 

Information:

 

US patent 8,193,180 is issued (06/05/2012)

 

Singh et al (2009). Invest New Drugs. Online pub.

Patent Information:
Category(s):
Oncology
For Information, Contact:
Margaret Shabashevich,
Manager of Operations
Technology Ventures Office
Brown University
401-863-7499 TVO_Patents@brown.edu
Inventors:
Rakesh Singh
Laurent Brard
Kyukwang Kim
Giselle Saulnier-Sholler
Thilo Lange
Keywords:
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