Detalles de la búsqueda
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.
Artículo
en Inglés
| MEDLINE | ID: mdl-35835377
2.
Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11ß-HSD1 using a scaffold-hopping approach.
Bioorg Med Chem Lett
; 69: 128782, 2022 08 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-35537608
3.
Parsaclisib Is a Next-Generation Phosphoinositide 3-Kinase δ Inhibitor with Reduced Hepatotoxicity and Potent Antitumor and Immunomodulatory Activities in Models of B-Cell Malignancy.
J Pharmacol Exp Ther
; 374(1): 211-222, 2020 07.
Artículo
en Inglés
| MEDLINE | ID: mdl-32345620
4.
Structures of full-length plasma kallikrein bound to highly specific inhibitors describe a new mode of targeted inhibition.
J Struct Biol
; 206(2): 170-182, 2019 05 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-30876891
5.
GBT440 increases haemoglobin oxygen affinity, reduces sickling and prolongs RBC half-life in a murine model of sickle cell disease.
Br J Haematol
; 175(1): 141-53, 2016 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-27378309
6.
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.
Artículo
en Inglés
| MEDLINE | ID: mdl-20363976
7.
Identification and characterization of INCB9471, an allosteric noncompetitive small-molecule antagonist of C-C chemokine receptor 5 with potent inhibitory activity against monocyte migration and HIV-1 infection.
J Pharmacol Exp Ther
; 338(1): 228-39, 2011 Jul.
Artículo
en Inglés
| MEDLINE | ID: mdl-21459966
8.
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.
Artículo
en Inglés
| MEDLINE | ID: mdl-21316220
9.
Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist.
Bioorg Med Chem Lett
; 21(5): 1442-6, 2011 Mar 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-21295478
10.
Discovery of ((1S,3R)-1-isopropyl-3-((3S,4S)-3-methoxy-tetrahydro-2H-pyran-4-ylamino)cyclopentyl)(4-(5-(trifluoromethyl)pyridazin-3-yl)piperazin-1-yl)methanone, PF-4254196, a CCR2 antagonist with an improved cardiovascular profile.
Bioorg Med Chem Lett
; 21(9): 2626-30, 2011 May 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-21315584
11.
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
Bioorg Med Chem Lett
; 20(24): 7473-8, 2010 Dec 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-21036044
12.
Discovery of novel selective HER-2 sheddase inhibitors through optimization of P1 moiety.
Bioorg Med Chem Lett
; 19(17): 5037-42, 2009 Sep 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-19635666
13.
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.
Artículo
en Inglés
| MEDLINE | ID: mdl-19457660
14.
INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ).
ACS Med Chem Lett
; 10(11): 1554-1560, 2019 Nov 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-31749910
15.
Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P1' permutations.
Bioorg Med Chem Lett
; 18(2): 560-4, 2008 Jan 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-18068976
16.
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.
Artículo
en Inglés
| MEDLINE | ID: mdl-18036818
17.
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.
Artículo
en Inglés
| MEDLINE | ID: mdl-17256836
18.
INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology.
ACS Med Chem Lett
; 8(5): 486-491, 2017 May 11.
Artículo
en Inglés
| MEDLINE | ID: mdl-28523098
19.
Discovery of GBT440, an Orally Bioavailable R-State Stabilizer of Sickle Cell Hemoglobin.
ACS Med Chem Lett
; 8(3): 321-326, 2017 Mar 09.
Artículo
en Inglés
| MEDLINE | ID: mdl-28337324
20.
Identification of ADAM10 as a major source of HER2 ectodomain sheddase activity in HER2 overexpressing breast cancer cells.
Cancer Biol Ther
; 5(6): 657-64, 2006 Jun.
Artículo
en Inglés
| MEDLINE | ID: mdl-16627989