R. Goldsmith

发表

Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.

Steve Price, E. Bradley, BinQing Wei, 2013, Journal of medicinal chemistry.

Highly potent non-peptidic inhibitors of the HCV NS3/NS4A serine protease.

J. Janc, N. Meanwell, K. Yeung, 2002, Bioorganic & medicinal chemistry letters.

Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.

BinQing Wei, D. Sutherlin, L. Friedman, 2011, Journal of medicinal chemistry.

Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer.

D. Sutherlin, S. Sideris, L. Friedman, 2010, Journal of medicinal chemistry.

Abstract DDT02-01: Discovery of GDC-0032: A beta-sparing PI3K inhibitor active against PIK3CA mutant tumors.

M. Belvin, E. Bradley, M. Ultsch, 2013 .

Tetrahydroindazoles as Interleukin-2 Inducible T-Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo.

P. McEwan, J. DeVoss, A. Zarrin, 2015, Journal of medicinal chemistry.

NMR determination of the major solution conformation of a peptoid pentamer with chiral side chains.

K A Dill, F E Cohen, E K Bradley, 1998, Proceedings of the National Academy of Sciences of the United States of America.

Sequence-specific polypeptoids: a diverse family of heteropolymers with stable secondary structure.

K A Dill, F E Cohen, E K Bradley, 1998, Proceedings of the National Academy of Sciences of the United States of America.

A Selective, Slow Binding Inhibitor of Factor VIIa Binds to a Nonstandard Active Site Conformation and Attenuates Thrombus Formation in Vivo*

D. Banner, M. Ultsch, D. Sutherlin, 2005, Journal of Biological Chemistry.

Cis-amide isosteric replacement in thienobenzoxepin inhibitors of PI3-kinase.

E. Bradley, BinQing Wei, J. Lesnick, 2013, Bioorganic & medicinal chemistry letters.

Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.

D. Sutherlin, S. Sideris, Leslie B. Lee, 2011, Bioorganic & medicinal chemistry letters.

Synthesis of N-substituted glycine peptoid libraries.

R. Zuckermann, G. Figliozzi, S. Banville, 1996, Methods in enzymology.

Rational design of phosphoinositide 3-kinase α inhibitors that exhibit selectivity over the phosphoinositide 3-kinase β isoform.

BinQing Wei, D. Sutherlin, J. Lesnick, 2011, Journal of medicinal chemistry.

Small molecule inhibition of GDC-0449 refractory smoothened mutants and downstream mechanisms of drug resistance.

Z. Modrušan, D. Sutherlin, T. Januario, 2011, Cancer research.

GDC-0449-a potent inhibitor of the hedgehog pathway.

K. Kotkow, L. Rubin, D. Sutherlin, 2009, Bioorganic & medicinal chemistry letters.

The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α.

S. Sideris, Leslie B. Lee, K. Edgar, 2012, Journal of medicinal chemistry.

New submonomers for poly N-substituted glycines (peptoids)

R. Zuckermann, T. Uno, E. Beausoleil, 1999 .

Corrigendum to “GDC-0449—A potent inhibitor of the hedgehog pathway” [Bioorg. Med. Chem. Lett. 19 (2009) 5576]

K. Kotkow, L. Rubin, D. Sutherlin, 2010 .