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Journal of Medicinal Chemistry|September 3, 2004
Design, synthesis, and biological evaluation of 1,2,3,7-tetrahydro-6h-purin-6-one and 3,7-dihydro-1h-purine-2,6-dione derivatives as corticotropin-releasing factor(1) receptor antagonistsRichard A Hartz, Kausik K Nanda, Charles L Ingalls, et al.Toxicological Sciences : an Official Journal of the Society of Toxicology|September 8, 2012
Toxicity profile of small-molecule IAP antagonist GDC-0152 is linked to TNF-α pharmacologyRebecca I Erickson, Jacqueline Tarrant, Gary Cain, et al.Journal of Medicinal Chemistry|June 11, 2015
Discovery of 1-{4-[3-fluoro-4-((3s,6r)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) inverse agonistBenjamin P Fauber, Olivier René, Yuzhong Deng, et al.Clinical Cancer Research : an Official Journal of the American Association for Cancer Research|January 20, 2022
First-in-Human Dose-Escalation Study of Cyclin-Dependent Kinase 9 Inhibitor VIP152 in Patients with Advanced Malignancies Shows Early Signs of Clinical EfficacyJennifer R Diamond, Valentina Boni, Emerson Lim, et al.Bioorganic & Medicinal Chemistry Letters|July 15, 2014
Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonistsBenjamin P Fauber, Olivier René, Gladys de Leon Boenig, et al.Clinical Cancer Research : an Official Journal of the American Association for Cancer Research|April 15, 2016
A Phase I Dose-Escalation Study Evaluating the Safety Tolerability and Pharmacokinetics of CUDC-427, a Potent, Oral, Monovalent IAP Antagonist, in Patients with Refractory Solid TumorsAnthony W Tolcher, Johanna C Bendell, Kyriakos P Papadopoulos, et al.ACS Medicinal Chemistry Letters|March 28, 2015
Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of ActionOlivier René, Benjamin P Fauber, Gladys de Leon Boenig, et al.Bioorganic & Medicinal Chemistry Letters|June 7, 2015
Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonistsBenjamin P Fauber, Alberto Gobbi, Kirk Robarge, et al.Clinical Cancer Research : an Official Journal of the American Association for Cancer Research|April 13, 2012
Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitorHarvey Wong, Laurent Vernillet, Amy Peterson, et al.Journal of Medicinal Chemistry|October 29, 2004
Synthesis, structure-activity relationships, and in vivo properties of 3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-ones as corticotropin-releasing factor-1 receptor antagonistsCarolyn D Dzierba, Amy G Takvorian, Maria Rafalski, et al.Pageof 11