Identification and optimization of tertiary sulfonamides as RORc inverse agonists

3^rd International Conference on Medicinal Chemistry & Computer Aided Drug Designing

December 08-10, 2014 DoubleTree by Hilton Hotel San Francisco Airport, USA

Benjamin P Fauber, Olivier René, Gladys de Leon Boenig, Brenda Burton, Yuzhong Deng, Celiné Eidenschenk, Christine Everett, Alberto Gobbi, Julie Hawkins, Sarah G Hymowitz, Adam R Johnson, Hank La, MaryaLiimatta, Peter Lockey, Maxine Norman, Wenjun Ouyang, Weiru Wang and Harvey Wong

Scientific Tracks Abstracts: Med Chem

Abstract :

Screening a nuclear receptor compound subset in a RORc biochemical binding assay revealed a benzylic tertiary sulfonamide hit. Using structure-based drug design principles, we created compounds with improved RORc biochemical inverse agonist activity and cellular potencies (<100 nM).These improved compounds also possessed appreciable selectivity for RORc over other nuclear receptors (>100-fold) and favorable physiochemical properties.

Biography :

Benjamin PFauber is a medicinal chemist at Genentech in South San Francisco, California. He earned his BSc from Colorado State University and PhD from the University of Texas at Austin. Prior to joining Genentech, he was employed by AstraZeneca and Array BioPharma as a medicinal chemist working in the areas of inflammatory disease and oncology.