55052-24-9Relevant articles and documents
Synthesis and structure?activity?relationship of 3,4?Diaryl?1H?pyrrolo[2,3?b]pyridines as irreversible Inhibitors of mutant EGFR?L858R/T790M
Günther, Marcel,Laux, Julian,Laufer, Stefan
, p. 91 - 96 (2019)
The epidermal growth factor receptor (EGFR) is a well?validated drug target for the treatment of non?small cell lung cancer. Here we present an optimization approach and preliminary structure?activity relationship for 1H?pyrrolo[2,3?b]pyridines as covalent irreversible mutant EGFR inhibitors. We synthesized a focused library to investigate the effect of different aromatic substituents in the 4?position of this scaffold, interacting with the gatekeeper. We determined the activity of the synthesized compounds mutant EGFR enzyme assays and determined the selectivity over the wild type.
Inhibitors of the Hippo Pathway Kinases STK3/MST2 and STK4/MST1 Have Utility for the Treatment of Acute Myeloid Leukemia
Bakas, Nicole A.,Bata, Nicole,Berger, Lena M.,Celeridad, Maria,Chaikuad, Apirat,Cosford, Nicholas D. P.,Dong, Jing,Knapp, Stefan,Lambert, Lester J.,Layng, Fabiana,Limpert, Allison S.,Liu, Guoxiong,Peng, Yi,Sheffler, Douglas J.,Wang, Li,Yuan, Cunxiang
, p. 1352 - 1369 (2021/12/06)
Serine/threonine-protein kinases 3 and 4 (STK3 and STK4, respectively) are key components of the Hippo signaling pathway, which regulates cell proliferation and death and provides a potential therapeutic target for acute myeloid leukemia (AML). Herein, we
AZAINDOLE CARBOXAMIDE COMPOUNDS FOR THE TREATMENT OF MYCOBACTERIAL INFECTIONS
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Page/Page column 271-272, (2021/04/02)
Provided herein are compounds of Formula (I) and Formula (II): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of tuberculosis.
MACROCYCLIC INHIBITORS OF PEPTIDYLARGININE DEIMINASES
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Page/Page column 188; 224-225, (2021/11/06)
The present disclosure relates to novel compounds for use in therapeutic treatement of a disease associated with peptidylarginine deiminases (PADs), such as peptidylarginine deiminase type 4 (PAD4). The present disclosure also relates to processes and intermediates for the preparation of such compounds, methods of using such compounds and pharmaceutical compositions comprising the compounds described herein.