Detalhe da pesquisa
1.
Discovery of novel spiro compound as RAF kinase inhibitor with in vitro potency against KRAS mutant cancer.
Bioorg Med Chem Lett
; 63: 128666, 2022 05 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-35276360
2.
Discovery of Potent Inhibitors of 11ß-Hydroxysteroid Dehydrogenase Type 1 Using a Novel Growth-Based Protocol of in Silico Screening and Optimization in CONTOUR.
J Chem Inf Model
; 59(8): 3422-3436, 2019 08 26.
Artigo
em Inglês
| MEDLINE | ID: mdl-31355641
3.
Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11ß hydroxysteroid dehydrogenase type 1 inhibitor.
Bioorg Med Chem
; 25(14): 3649-3657, 2017 07 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-28528082
4.
Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.
Bioorg Med Chem Lett
; 26(20): 5044-5050, 2016 10 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-27599745
5.
Discovery of Isoindoline Amide Derivatives as Potent and Orally Bioavailable ADAMTS-4/5 Inhibitors for the Treatment of Osteoarthritis.
ACS Pharmacol Transl Sci
; 5(7): 458-467, 2022 Jul 08.
Artigo
em Inglês
| MEDLINE | ID: mdl-35837136
6.
Novel Small Molecule Tyrosine Kinase 2 Pseudokinase Ligands Block Cytokine-Induced TYK2-Mediated Signaling Pathways.
Front Immunol
; 13: 884399, 2022.
Artigo
em Inglês
| MEDLINE | ID: mdl-35693820
7.
SHR1032, a novel STING agonist, stimulates anti-tumor immunity and directly induces AML apoptosis.
Sci Rep
; 12(1): 8579, 2022 05 20.
Artigo
em Inglês
| MEDLINE | ID: mdl-35595822
8.
Discovery of spiro amide SHR902275: A potent, selective, and efficacious RAF inhibitor targeting RAS mutant cancers.
Eur J Med Chem
; 228: 114040, 2022 Jan 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-34906761
9.
A Novel CD73 Inhibitor SHR170008 Suppresses Adenosine in Tumor and Enhances Anti-Tumor Activity with PD-1 Blockade in a Mouse Model of Breast Cancer.
Onco Targets Ther
; 14: 4561-4574, 2021.
Artigo
em Inglês
| MEDLINE | ID: mdl-34466002
10.
Discovery and optimization of adamantyl carbamate inhibitors of 11ß-HSD1.
Bioorg Med Chem Lett
; 20(22): 6725-9, 2010 Nov 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-20864344
11.
Spirocyclic ureas: orally bioavailable 11 beta-HSD1 inhibitors identified by computer-aided drug design.
Bioorg Med Chem Lett
; 20(3): 881-6, 2010 Feb 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-20064717
12.
Spongipyran Synthetic Studies. Total Synthesis of (+)-Spongistatin 2.
Tetrahedron
; 65(33): 6470-6488, 2009 Aug 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-20161196
13.
Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) ß Agonist.
J Med Chem
; 59(7): 3264-71, 2016 Apr 14.
Artigo
em Inglês
| MEDLINE | ID: mdl-26990539
14.
Pharmacological characterization of the selective 11ß-hydroxysteroid dehydrogenase 1 inhibitor, BI 135585, a clinical candidate for the treatment of type 2 diabetes.
Eur J Pharmacol
; 746: 50-5, 2015 Jan 05.
Artigo
em Inglês
| MEDLINE | ID: mdl-25445047
15.
Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells.
J Med Chem
; 46(4): 453-6, 2003 Feb 13.
Artigo
em Inglês
| MEDLINE | ID: mdl-12570367
16.
The medicinal chemistry of liver X receptor (LXR) modulators.
J Med Chem
; 57(17): 7182-205, 2014 Sep 11.
Artigo
em Inglês
| MEDLINE | ID: mdl-24832115
17.
Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11ß-hydroxysteroid dehydrogenase type 1.
J Med Chem
; 54(17): 6050-62, 2011 Sep 08.
Artigo
em Inglês
| MEDLINE | ID: mdl-21786805
18.
The Spongistatins: Architecturally Complex Natural Products-Part Two: Synthesis of the C(29-51) Subunit, Fragment Assembly, and Final Elaboration to (+)-Spongistatin 2 Financial support was provided by the National Institutes of Health (National Cancer Institute) through Grant CA-70329, a NIH Postdoctoral Fellowship to C.S.B., a Japan Society for Promotion of Science Fellowship to N.M., and a Royal Society Fulbright Fellowship to V.A.D. We also thank the Daiichi Pharmaceutical Co., Ltd, and the Tanabe Seiyaku Co., Ltd for financial support. Finally we thank Dr George T. Furst, Dr. Patrick J. Carroll, and Dr. Rakesh Kohli of the University of Pennsylvania Spectroscopic Service Center for assistance in securing and interpreting high-field NMR spectra, X-ray crystal structures, and mass spectra, respectively.
Angew Chem Int Ed Engl
; 40(1): 196-199, 2001 Jan 05.
Artigo
em Inglês
| MEDLINE | ID: mdl-11169711
19.
The Spongistatins: Architecturally Complex Natural Products-Part Two: Synthesis of the C(29-51) Subunit, Fragment Assembly, and Final Elaboration to (+)-Spongistatin 2.
Angew Chem Int Ed Engl
; 40(1): 196-199, 2001 Jan 05.
Artigo
em Inglês
| MEDLINE | ID: mdl-29711943
20.
The Spongistatins: Architecturally Complex Natural Products-Part One: A Formal Synthesis of (+)-Spongistatin 1 by Construction of an Advanced ABCD Fragment Financial support was provided by the National Institutes of Health (National Cancer Institute) through Grant CA-70329, NIH Postdoctoral Fellowships to A.M.B. and W.H.M., a Japan Society for Promotion of Science Fellowship to N.M., and a Royal Society Fulbright Fellowship to V.A.D. We also thank the Daiichi Pharmaceutical Co., Ltd, and the Tanabe Seiyaku Co., Ltd for financial support. Finally we thank Dr. George T. Furst, Dr. Patrick J. Carroll, Dr. Rakesh Kohli, and Mr John Dykins of the University of Pennsylvania Spectroscopic Service Center for assistance in securing and interpreting high-field NMR spectra, X-ray crystal structures, and mass spectra.
Angew Chem Int Ed Engl
; 40(1): 191-195, 2001 Jan 05.
Artigo
em Inglês
| MEDLINE | ID: mdl-11169710