Detalhe da pesquisa
1.
Stereoselective Amine Synthesis Mediated by a Zirconocene Hydride to Accelerate a Drug Discovery Program.
J Org Chem
; 89(6): 3875-3882, 2024 03 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-38422508
2.
Design and evaluation of achiral, non-atropisomeric 4-(aminomethyl)phthalazin-1(2H)-one derivatives as novel PRMT5/MTA inhibitors.
Bioorg Med Chem
; 71: 116947, 2022 10 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-35926325
3.
Discovery of Five SOS2 Fragment Hits with Binding Modes Determined by SOS2 X-Ray Cocrystallography.
J Med Chem
; 67(1): 774-781, 2024 Jan 11.
Artigo
em Inglês
| MEDLINE | ID: mdl-38156904
4.
The SOS1 Inhibitor MRTX0902 Blocks KRAS Activation and Demonstrates Antitumor Activity in Cancers Dependent on KRAS Nucleotide Loading.
Mol Cancer Ther
; 2024 Apr 19.
Artigo
em Inglês
| MEDLINE | ID: mdl-38641404
5.
Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein.
J Med Chem
; 67(6): 4936-4949, 2024 Mar 28.
Artigo
em Inglês
| MEDLINE | ID: mdl-38477582
6.
Discovery and synthesis of novel 4-aminopyrrolopyrimidine Tie-2 kinase inhibitors for the treatment of solid tumors.
Bioorg Med Chem Lett
; 23(10): 3059-63, 2013 May 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-23566514
7.
Optimization of mTOR Inhibitors Using Property-Based Drug Design and Free-Wilson Analysis for Improved In Vivo Efficacy.
ACS Med Chem Lett
; 14(11): 1544-1550, 2023 Nov 09.
Artigo
em Inglês
| MEDLINE | ID: mdl-37970587
8.
MRTX1719 Is an MTA-Cooperative PRMT5 Inhibitor That Exhibits Synthetic Lethality in Preclinical Models and Patients with MTAP-Deleted Cancer.
Cancer Discov
; 13(11): 2412-2431, 2023 11 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-37552839
9.
Atropisomeric Racemization Kinetics of MRTX1719 Using Chiral Solvating Agent-Assisted 19F NMR Spectroscopy.
ACS Omega
; 7(36): 32062-32067, 2022 Sep 13.
Artigo
em Inglês
| MEDLINE | ID: mdl-36120049
10.
Fragment optimization and elaboration strategies - the discovery of two lead series of PRMT5/MTA inhibitors from five fragment hits.
RSC Med Chem
; 13(12): 1549-1564, 2022 Dec 14.
Artigo
em Inglês
| MEDLINE | ID: mdl-36545438
11.
Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5â¢MTA Complex for the Treatment of MTAP-Deleted Cancers.
J Med Chem
; 65(3): 1749-1766, 2022 02 10.
Artigo
em Inglês
| MEDLINE | ID: mdl-35041419
12.
Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein-Protein Interaction.
J Med Chem
; 65(14): 9678-9690, 2022 07 28.
Artigo
em Inglês
| MEDLINE | ID: mdl-35833726
13.
Anti-tumor efficacy of a potent and selective non-covalent KRASG12D inhibitor.
Nat Med
; 28(10): 2171-2182, 2022 Oct.
Artigo
em Inglês
| MEDLINE | ID: mdl-36216931
14.
Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor.
J Med Chem
; 65(4): 3123-3133, 2022 02 24.
Artigo
em Inglês
| MEDLINE | ID: mdl-34889605
15.
4-methylpteridinones as orally active and selective PI3K/mTOR dual inhibitors.
Bioorg Med Chem Lett
; 20(20): 6096-9, 2010 Oct 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-20817449
16.
The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients.
Cancer Discov
; 10(1): 54-71, 2020 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-31658955
17.
Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer.
J Med Chem
; 63(13): 6679-6693, 2020 07 09.
Artigo
em Inglês
| MEDLINE | ID: mdl-32250617
18.
2-Morpholino-4-oxo-4,5-dihydro-thio-phene-3-carbonitrile.
Acta Crystallogr Sect E Struct Rep Online
; 65(Pt 11): o2765, 2009 Oct 17.
Artigo
em Inglês
| MEDLINE | ID: mdl-21578359
19.
Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity.
ACS Med Chem Lett
; 9(12): 1230-1234, 2018 Dec 13.
Artigo
em Inglês
| MEDLINE | ID: mdl-30613331
20.
Pharmacological characterization of CP-547,632, a novel vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for cancer therapy.
Cancer Res
; 63(21): 7301-9, 2003 Nov 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-14612527