869335-73-9Relevant articles and documents
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
Cu(II)-catalyzed sulfonylation of 7-azaindoles using DABSO as SO2-Source and its mechanistic study
Urvashi,Dar, Mohammad Ovais,Bharatam, Prasad V.,Das, Parthasarathi,Kukreti, Shrikant,Tandon, Vibha
, (2020/06/23)
DABSO mediated sulfonylation of iodinated 7-azaindoles was achieved for the first time through sulfonylative Suzuki-Miyaura cross coupling (SMC) reaction under mild conditions giving good yields of sulfonylated 7-azaindole derivatives. Interestingly, control experiments suggest that present method involves in-situ generation of ArSO2 free radical followed by the key steps of SMC reaction. Scope of the reaction was explored with both electronically different and bulky group carrying boronic acids as coupling partner. The sulfonylation is scalable and occurred selectively at iodo group, irrespective of its position on azaindole. Moreover, the proposed mechanism has been supported by electron paramagnetic resonance (EPR) and density functional theory (DFT) calculations.
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 (2018/12/04)
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.