Detalhe da pesquisa
1.
Discovery of ASP6918, a KRAS G12C inhibitor: Synthesis and structure-activity relationships of 1-{2,7-diazaspiro[3.5]non-2-yl}prop-2-en-1-one derivatives as covalent inhibitors with good potency and oral activity for the treatment of solid tumors.
Bioorg Med Chem
; 98: 117581, 2024 Jan 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-38176113
2.
Discovery and biological evaluation of 1-{2,7-diazaspiro[3.5]nonan-2-yl}prop-2-en-1-one derivatives as covalent inhibitors of KRAS G12C with favorable metabolic stability and anti-tumor activity.
Bioorg Med Chem
; 71: 116949, 2022 10 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-35926326
3.
Synthesis and structure-activity relationships of pyrimidine derivatives as potent and orally active FGFR3 inhibitors with both increased systemic exposure and enhanced in vitro potency.
Bioorg Med Chem
; 33: 116019, 2021 03 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-33486159
4.
Structure-based drug design of 1,3,5-triazine and pyrimidine derivatives as novel FGFR3 inhibitors with high selectivity over VEGFR2.
Bioorg Med Chem
; 28(10): 115453, 2020 05 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-32278710
5.
Synthesis, SAR study, and biological evaluation of novel 2,3-dihydro-1H-imidazo[1,2-a]benzimidazole derivatives as phosphodiesterase 10A inhibitors.
Bioorg Med Chem
; 27(16): 3692-3706, 2019 08 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-31301949
6.
Discovery and structural characterization of peficitinib (ASP015K) as a novel and potent JAK inhibitor.
Bioorg Med Chem
; 26(18): 4971-4983, 2018 10 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-30145050
7.
Fragment-Based Discovery of Pyrimido[1,2-b]indazole PDE10A Inhibitors.
Chem Pharm Bull (Tokyo)
; 66(3): 286-294, 2018.
Artigo
em Inglês
| MEDLINE | ID: mdl-29491261
8.
Structures of complexes of type 5 17ß-hydroxysteroid dehydrogenase with structurally diverse inhibitors: insights into the conformational changes upon inhibitor binding.
Acta Crystallogr D Biol Crystallogr
; 71(Pt 4): 918-27, 2015 Apr.
Artigo
em Inglês
| MEDLINE | ID: mdl-25849402
9.
Structural insights into the novel inhibition mechanism of Trypanosoma cruzi spermidine synthase.
Acta Crystallogr D Biol Crystallogr
; 71(Pt 9): 1879-89, 2015 Sep.
Artigo
em Inglês
| MEDLINE | ID: mdl-26327378
10.
Identification of N-ethylmethylamine as a novel scaffold for inhibitors of soluble epoxide hydrolase by crystallographic fragment screening.
Bioorg Med Chem
; 23(10): 2310-7, 2015 May 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-25862210
11.
Addressing phototoxicity observed in a novel series of biaryl derivatives: discovery of potent, selective and orally active phosphodiesterase 10A inhibitor ASP9436.
Bioorg Med Chem
; 23(13): 3351-67, 2015 Jul 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-25960322
12.
Synthesis, SAR study, and biological evaluation of novel quinoline derivatives as phosphodiesterase 10A inhibitors with reduced CYP3A4 inhibition.
Bioorg Med Chem
; 23(2): 297-313, 2015 Jan 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-25515954
13.
Structural insights into binding of inhibitors to soluble epoxide hydrolase gained by fragment screening and X-ray crystallography.
Bioorg Med Chem
; 22(8): 2427-34, 2014 Apr 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-24656800
14.
Novel benzimidazole derivatives as phosphodiesterase 10A (PDE10A) inhibitors with improved metabolic stability.
Bioorg Med Chem
; 22(13): 3515-26, 2014 Jul 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-24837154
15.
Design and synthesis of novel benzimidazole derivatives as phosphodiesterase 10A inhibitors with reduced CYP1A2 inhibition.
Bioorg Med Chem
; 21(24): 7612-23, 2013 Dec 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-24238902
16.
Discovery of a Hidden Trypanosoma cruzi Spermidine Synthase Binding Site and Inhibitors through In Silico, In Vitro, and X-ray Crystallography.
ACS Omega
; 8(29): 25850-25860, 2023 Jul 25.
Artigo
em Inglês
| MEDLINE | ID: mdl-37521650
17.
Unique "delta lock" structure of telmisartan is involved in its strongest binding affinity to angiotensin II type 1 receptor.
Biochem Biophys Res Commun
; 404(1): 434-7, 2011 Jan 07.
Artigo
em Inglês
| MEDLINE | ID: mdl-21130741
18.
Effect of Fms-like tyrosine kinase 3 (FLT3) ligand (FL) on antitumor activity of gilteritinib, a FLT3 inhibitor, in mice xenografted with FL-overexpressing cells.
Oncotarget
; 10(58): 6111-6123, 2019 Oct 22.
Artigo
em Inglês
| MEDLINE | ID: mdl-31692922
19.
In silico, in vitro, X-ray crystallography, and integrated strategies for discovering spermidine synthase inhibitors for Chagas disease.
Sci Rep
; 7(1): 6666, 2017 07 27.
Artigo
em Inglês
| MEDLINE | ID: mdl-28751689
20.
Structural basis for telmisartan-mediated partial activation of PPAR gamma.
Hypertens Res
; 35(7): 715-9, 2012 Jul.
Artigo
em Inglês
| MEDLINE | ID: mdl-22357520