Detalhe da pesquisa
1.
Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2.
Proc Natl Acad Sci U S A;
121(6): e2317756121, 2024 Feb 06.
Artigo
em Inglês
| MEDLINE
| ID: mdl-38300868
2.
1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of NaV1.7 inhibition.
Bioorg Med Chem Lett;
28(11): 2103-2108, 2018 06 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-29709252
3.
The discovery of benzoxazine sulfonamide inhibitors of NaV1.7: Tools that bridge efficacy and target engagement.
Bioorg Med Chem Lett;
27(15): 3477-3485, 2017 08 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-28629594
4.
Development of novel azabenzofuran TRPA1 antagonists as in vivo tools.
Bioorg Med Chem Lett;
24(15): 3464-8, 2014 Aug 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-24953819
5.
Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia.
Cancer Discov;
14(2): 240-257, 2024 Feb 08.
Artigo
em Inglês
| MEDLINE
| ID: mdl-37916956
6.
Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors.
Bioorg Med Chem Lett;
22(12): 4089-93, 2012 Jun 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-22595176
7.
Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors.
Bioorg Med Chem Lett;
22(15): 4967-74, 2012 Aug 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-22765895
8.
Discovery of triazine-benzimidazoles as selective inhibitors of mTOR.
Bioorg Med Chem Lett;
21(7): 2064-70, 2011 Apr 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-21376583
9.
Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors.
Bioorg Med Chem Lett;
19(22): 6307-12, 2009 Nov 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-19819693
10.
Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase.
J Med Chem;
51(10): 2879-82, 2008 May 22.
Artigo
em Inglês
| MEDLINE
| ID: mdl-18426196
11.
Chemical reactivity of methoxy 4-o-aryl quinolines: identification of glutathione displacement products in vitro and in vivo.
Chem Res Toxicol;
21(11): 2216-22, 2008 Nov.
Artigo
em Inglês
| MEDLINE
| ID: mdl-18837519
12.
Synthesis and activity of substituted carbamates as potentiators of the alpha4beta2 nicotinic acetylcholine receptor.
Bioorg Med Chem Lett;
18(20): 5643-7, 2008 Oct 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-18805006
13.
Discovery and optimization of substituted piperidines as potent, selective, CNS-penetrant alpha4beta2 nicotinic acetylcholine receptor potentiators.
Bioorg Med Chem Lett;
18(19): 5209-12, 2008 Oct 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-18789861
14.
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity.
J Med Chem;
60(14): 5990-6017, 2017 07 27.
Artigo
em Inglês
| MEDLINE
| ID: mdl-28324649
15.
Direct, Regioselective N-Alkylation of 1,3-Azoles.
Org Lett;
18(1): 16-9, 2016 Jan 04.
Artigo
em Inglês
| MEDLINE
| ID: mdl-26671035
16.
Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity.
J Med Chem;
59(6): 2794-809, 2016 Mar 24.
Artigo
em Inglês
| MEDLINE
| ID: mdl-26942860
17.
Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity.
J Med Chem;
59(6): 2328-42, 2016 Mar 24.
Artigo
em Inglês
| MEDLINE
| ID: mdl-26812066
18.
Structure-based design of novel class II c-Met inhibitors: 2. SAR and kinase selectivity profiles of the pyrazolone series.
J Med Chem;
55(5): 1868-97, 2012 Mar 08.
Artigo
em Inglês
| MEDLINE
| ID: mdl-22320327
19.
Tetraarylphosphonium salts as solubility-control groups: phosphonium-supported triphenylphosphine and azodicarboxylate reagents.
Angew Chem Int Ed Engl;
45(9): 1415-20, 2006 Feb 20.
Artigo
em Inglês
| MEDLINE
| ID: mdl-16425329
20.
Efficient total syntheses of (-)-colombiasin A and (-)-elisapterosin B: application of the Cr-catalyzed asymmetric quinone Diels-Alder reaction.
Angew Chem Int Ed Engl;
44(37): 6046-50, 2005 Sep 19.
Artigo
em Inglês
| MEDLINE
| ID: mdl-16108082