Detalhe da pesquisa
1.
Small-molecule factor D inhibitors targeting the alternative complement pathway.
Nat Chem Biol
; 12(12): 1105-1110, 2016 Dec.
Artigo
em Inglês
| MEDLINE | ID: mdl-27775713
2.
trans-(3S,4S)-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part I: prime site exploration using an amino linker.
Bioorg Med Chem Lett
; 25(8): 1782-1786, 2015 Apr 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-25782742
3.
trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker.
Bioorg Med Chem Lett
; 25(8): 1787-1791, 2015 Apr 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-25754490
4.
Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C.
Cancer Discov
; 12(6): 1500-1517, 2022 06 02.
Artigo
em Inglês
| MEDLINE | ID: mdl-35404998
5.
JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors.
J Med Chem
; 65(24): 16173-16203, 2022 12 22.
Artigo
em Inglês
| MEDLINE | ID: mdl-36399068
6.
Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach.
J Med Chem
; 63(15): 8088-8113, 2020 08 13.
Artigo
em Inglês
| MEDLINE | ID: mdl-32551603
7.
Design, Synthesis, and Preclinical Characterization of Selective Factor D Inhibitors Targeting the Alternative Complement Pathway.
J Med Chem
; 62(9): 4656-4668, 2019 05 09.
Artigo
em Inglês
| MEDLINE | ID: mdl-30995036
8.
Discovery and Design of First Benzylamine-Based Ligands Binding to an Unlocked Conformation of the Complement Factor D.
ACS Med Chem Lett
; 9(5): 490-495, 2018 May 10.
Artigo
em Inglês
| MEDLINE | ID: mdl-29795765
9.
Structure-Based Library Design and Fragment Screening for the Identification of Reversible Complement Factor D Protease Inhibitors.
J Med Chem
; 60(5): 1946-1958, 2017 03 09.
Artigo
em Inglês
| MEDLINE | ID: mdl-28157311
10.
Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo.
J Med Chem
; 60(13): 5717-5735, 2017 07 13.
Artigo
em Inglês
| MEDLINE | ID: mdl-28621538
11.
Amino Zinc Enolate Carbocyclization Reactions. New Access to Polysubstituted Piperidine Derivatives.
J Org Chem
; 63(3): 566-574, 1998 Feb 06.
Artigo
em Inglês
| MEDLINE | ID: mdl-11672046
12.
Diastereoselective and Enantioselective Intramolecular Amino-Zinc-Enolate Carbometalation Reactions. A New Polysubstituted Pyrrolidines Synthesis.
J Org Chem
; 63(8): 2442-2450, 1998 Apr 17.
Artigo
em Inglês
| MEDLINE | ID: mdl-11672102
13.
Fluorescence Lifetime-Based Competitive Binding Assays for Measuring the Binding Potency of Protease Inhibitors In Vitro.
J Biomol Screen
; 19(6): 870-7, 2014 Jul.
Artigo
em Inglês
| MEDLINE | ID: mdl-24487225
14.
The discovery of novel potent trans-3,4-disubstituted pyrrolidine inhibitors of the human aspartic protease renin from in silico three-dimensional (3D) pharmacophore searches.
J Med Chem
; 56(6): 2207-17, 2013 Mar 28.
Artigo
em Inglês
| MEDLINE | ID: mdl-23425156
15.
A sensitive fluorescence intensity assay for deubiquitinating proteases using ubiquitin-rhodamine110-glycine as substrate.
Anal Biochem
; 371(2): 201-7, 2007 Dec 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-17869210
16.
Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 1.
Bioorg Med Chem Lett
; 14(18): 4623-6, 2004 Sep 20.
Artigo
em Inglês
| MEDLINE | ID: mdl-15324876
17.
Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: design, synthesis and structure-activity relationship studies.
Bioorg Med Chem Lett
; 14(18): 4607-13, 2004 Sep 20.
Artigo
em Inglês
| MEDLINE | ID: mdl-15324874
18.
Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 2: metabolism-directed optimization studies towards orally bioavailable derivatives.
Bioorg Med Chem Lett
; 14(18): 4615-21, 2004 Sep 20.
Artigo
em Inglês
| MEDLINE | ID: mdl-15324875
19.
Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 2: Optimization of 5,8-disubstituted derivatives.
Bioorg Med Chem Lett
; 14(18): 4627-31, 2004 Sep 20.
Artigo
em Inglês
| MEDLINE | ID: mdl-15324877