Detalhe da pesquisa
1.
Discovery of a novel 2-spiroproline steroid mimetic scaffold for the potent inhibition of 11ß-HSD1.
Bioorg Med Chem Lett
; 73: 128884, 2022 10 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-35835377
2.
Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050.
J Immunol
; 184(9): 5298-307, 2010 May 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-20363976
3.
Design and synthesis of novel CCR2 antagonists: investigation of non-aryl/heteroaryl binding motifs.
Bioorg Med Chem Lett
; 21(6): 1827-31, 2011 Mar 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-21316220
4.
Pharmacological characterization of INCB3344, a small molecule antagonist of human CCR2.
Biochem Biophys Res Commun
; 387(2): 251-5, 2009 Sep 18.
Artigo
em Inglês
| MEDLINE | ID: mdl-19576173
5.
Discovery of novel selective HER-2 sheddase inhibitors through optimization of P1 moiety.
Bioorg Med Chem Lett
; 19(17): 5037-42, 2009 Sep 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-19635666
6.
Compelling P1 substituent affect on metalloprotease binding profile enables the design of a novel cyclohexyl core scaffold with excellent MMP selectivity and HER-2 sheddase inhibition.
Bioorg Med Chem Lett
; 19(13): 3525-30, 2009 Jul 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-19457660
7.
Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE): discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1' substituents.
Bioorg Med Chem Lett
; 18(6): 1958-62, 2008 Mar 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-18282708
8.
Potent, exceptionally selective, orally bioavailable inhibitors of TNF-alpha Converting Enzyme (TACE): novel 2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamide P1' substituents.
Bioorg Med Chem Lett
; 18(5): 1577-82, 2008 Mar 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-18242982
9.
Alpha,Beta-cyclic-beta-benzamido hydroxamic acids: Novel oxaspiro[4.4]nonane templates for the discovery of potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Bioorg Med Chem Lett
; 18(4): 1288-92, 2008 Feb 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-18234496
10.
Alpha,beta-cyclic-beta-benzamido hydroxamic acids: novel templates for the design, synthesis, and evaluation of selective inhibitors of TNF-alpha converting enzyme (TACE).
Bioorg Med Chem Lett
; 18(2): 694-9, 2008 Jan 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-18061445
11.
Discovery of beta-benzamido hydroxamic acids as potent, selective, and orally bioavailable TACE inhibitors.
Bioorg Med Chem Lett
; 18(1): 241-6, 2008 Jan 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-18032037
12.
Design and identification of selective HER-2 sheddase inhibitors via P1' manipulation and unconventional P2' perturbations to induce a molecular metamorphosis.
Bioorg Med Chem Lett
; 18(1): 159-63, 2008 Jan 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-18036818
13.
Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.
J Med Chem
; 50(4): 603-6, 2007 Feb 22.
Artigo
em Inglês
| MEDLINE | ID: mdl-17256836
14.
Sultam hydroxamates as novel matrix metalloproteinase inhibitors.
J Med Chem
; 47(12): 2981-3, 2004 Jun 03.
Artigo
em Inglês
| MEDLINE | ID: mdl-15163180
15.
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
J Med Chem
; 45(23): 4954-7, 2002 Nov 07.
Artigo
em Inglês
| MEDLINE | ID: mdl-12408705
16.
Design, synthesis, and evaluation of benzothiadiazepine hydroxamates as selective tumor necrosis factor-alpha converting enzyme inhibitors.
J Med Chem
; 46(10): 1811-23, 2003 May 08.
Artigo
em Inglês
| MEDLINE | ID: mdl-12723945
17.
Discovery of low nanomolar non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Bioorg Med Chem Lett
; 17(1): 266-71, 2007 Jan 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-17027261
18.
Discovery of novel hydantoins as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Bioorg Med Chem Lett
; 17(5): 1413-7, 2007 Mar 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-17188863
19.
Pharmacokinetics and pharmacodynamics of DPC 333 ((2R)-2-((3R)-3-amino-3{4-[2-methyl-4-quinolinyl) methoxy] phenyl}-2-oxopyrrolidinyl)-N-hydroxy-4-methylpentanamide)), a potent and selective inhibitor of tumor necrosis factor alpha-converting enzyme in rodents, dogs, chimpanzees, and humans.
Drug Metab Dispos
; 35(10): 1916-25, 2007 Oct.
Artigo
em Inglês
| MEDLINE | ID: mdl-17656469
20.
A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1' group for the beta-amino hydroxamic acid derived TACE inhibitors.
Bioorg Med Chem Lett
; 17(7): 1865-70, 2007 Apr 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-17276676