Detalles de la búsqueda
1.
Preclinical characterization of the absorption and disposition of the brain penetrant PI3K/mTOR inhibitor paxalisib and prediction of its pharmacokinetics and efficacy in human.
Xenobiotica
; 54(2): 64-74, 2024 Feb.
Artículo
en Inglés
| MEDLINE | ID: mdl-38197324
2.
Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma.
Drug Metab Dispos
; 44(12): 1881-1889, 2016 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-27638506
3.
Distribution of the phosphatidylinositol 3-kinase inhibitors Pictilisib (GDC-0941) and GNE-317 in U87 and GS2 intracranial glioblastoma models-assessment by matrix-assisted laser desorption ionization imaging.
Drug Metab Dispos
; 42(7): 1110-6, 2014 Jul.
Artículo
en Inglés
| MEDLINE | ID: mdl-24754926
4.
Cis-amide isosteric replacement in thienobenzoxepin inhibitors of PI3-kinase.
Bioorg Med Chem Lett
; 23(3): 897-901, 2013 Feb 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-23265894
5.
Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase ß isoform.
Bioorg Med Chem Lett
; 23(9): 2606-13, 2013 May 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-23540645
6.
Preclinical assessment of the absorption and disposition of the phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor GDC-0980 and prediction of its pharmacokinetics and efficacy in human.
Drug Metab Dispos
; 40(9): 1785-96, 2012 Sep.
Artículo
en Inglés
| MEDLINE | ID: mdl-22696419
7.
RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy.
Cancer Discov
; 12(1): 204-219, 2022 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-34544753
8.
Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.
Bioorg Med Chem Lett
; 21(13): 4054-8, 2011 Jul 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-21636270
9.
Preclinical pharmacokinetics of the novel PI3K inhibitor GDC-0941 and prediction of its pharmacokinetics and efficacy in human.
Xenobiotica
; 41(12): 1088-99, 2011 Dec.
Artículo
en Inglés
| MEDLINE | ID: mdl-21838594
10.
Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.
Bioorg Med Chem Lett
; 20(20): 6048-51, 2010 Oct 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-20822905
11.
Multiparametric MR-PET Imaging Predicts Pharmacokinetics and Clinical Response to GDC-0084 in Patients with Recurrent High-Grade Glioma.
Clin Cancer Res
; 26(13): 3135-3144, 2020 07 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-32269051
12.
First-in-Human Phase I Study to Evaluate the Brain-Penetrant PI3K/mTOR Inhibitor GDC-0084 in Patients with Progressive or Recurrent High-Grade Glioma.
Clin Cancer Res
; 26(8): 1820-1828, 2020 04 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-31937616
13.
Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.
ACS Med Chem Lett
; 7(4): 351-6, 2016 Apr 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-27096040
14.
The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).
J Med Chem
; 59(3): 985-1002, 2016 Feb 11.
Artículo
en Inglés
| MEDLINE | ID: mdl-26741947
15.
Inhibitors of Tissue Factor. Factor VIIa for anticoagulant therapy.
Curr Med Chem
; 11(17): 2275-90, 2004 Sep.
Artículo
en Inglés
| MEDLINE | ID: mdl-15379712
16.
Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a ß-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.
J Med Chem
; 56(11): 4597-610, 2013 Jun 13.
Artículo
en Inglés
| MEDLINE | ID: mdl-23662903
17.
The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α.
J Med Chem
; 55(18): 8007-20, 2012 Sep 27.
Artículo
en Inglés
| MEDLINE | ID: mdl-22946614
18.
Targeting the PI3K pathway in the brain--efficacy of a PI3K inhibitor optimized to cross the blood-brain barrier.
Clin Cancer Res
; 18(22): 6239-48, 2012 Nov 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-22992516
19.
GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway.
Mol Cancer Ther
; 10(12): 2426-36, 2011 Dec.
Artículo
en Inglés
| MEDLINE | ID: mdl-21998291
20.
The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer .
J Med Chem
; 51(18): 5522-32, 2008 Sep 25.
Artículo
en Inglés
| MEDLINE | ID: mdl-18754654