68774-78-7Relevant academic research and scientific papers
PYRIDAZINIUM COMPOUNDS FOR USE IN CONTROLLING UNWANTED PLANT GROWTH
-
Page/Page column 57-58, (2020/08/22)
Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as pesticides, especially as herbicides.
Discovery of [1,2,4]triazolo[4,3-a]pyrazine derivatives bearing a 4-oxo-pyridazinone moiety as potential c-Met kinase inhibitors
Liu, Xiaobo,Sun, Xin,Xiong, Hehua,Xu, Shan,Yang, Zunhua,Zhang, Binliang,Zhang, Qian,Zheng, Pengwu,Zhu, Wufu
, p. 9053 - 9063 (2020/06/08)
Two series of [1,2,4]triazolo[4,3-a]pyrazine derivatives bearing 4-oxo-pyridazinone moieties (compounds21a-land22a-l) were designed and their IC50values were evaluated against three cancer cell lines (A549, MCF-7 and HeLa) and c-Met kinase. Among them, the compound with most potential,22i,exhibited excellent anti-tumor activity against A549, MCF-7 and HeLa cancer cell lines with IC50values of 0.83 ± 0.07 μM, 0.15 ± 0.08 μM and 2.85 ± 0.74 μM, respectively, and it also possessed superior c-Met kinase inhibition ability at the nanomolar level (IC50= 48 nM). Moreover, dose-dependent experiments, AO fluorescence staining, cell cycle assay, Annexin V-FITC/PI staining and docking studies were carried out in this study. The results demonstrated that compound22icould be a potential c-Met kinase inhibitor.
Triazolo pyrazine compound containing heteroaryl substituted pyridazinone structure, and preparation method and applications thereof
-
Paragraph 0131-0134, (2019/11/29)
The invention relates to a triazolo pyrazine compound containing a heteroaryl substituted pyridazinone structure, and pharmaceutically acceptable salts, hydrates, solvates, and a prodrug thereof, wherein the triazolo pyrazine compound containing a heteroa
Discovery of novel [1,2,4]triazolo[4,3-a]quinoxaline aminophenyl derivatives as BET inhibitors for cancer treatment
Ali, Imran,Lee, Jooyun,Go, Areum,Choi, Gildon,Lee, Kwangho
, p. 4606 - 4613 (2017/09/29)
Bromodomain and extra-terminal (BET) proteins, a class of epigenetic reader domains has emerged as a promising new target class for small molecule drug discovery for the treatment of cancer, inflammatory, and autoimmune diseases. Starting from in silico screening campaign, herein we report the discovery of novel BET inhibitors based on [1,2,4]triazolo[4,3-a]quinoxaline scaffold and their biological evaluation. The hit compound was optimized using the medicinal chemistry approach to the lead compound with excellent inhibitory activities against BRD4 in the binding assay. The substantial antiproliferative activities in human cancer cell lines, promising drug-like properties, and the selectivity for the BET family make the lead compound (13) as a novel BRD4 inhibitor motif for anti-cancer drug discovery.
BICYCLIC AZAHETEROCYCLIC COMPOUNDS AS NR2B NMDA RECEPTOR ANTAGONISTS
-
Paragraph 0197, (2016/07/05)
Disclosed are chemical entities of Formula (I): wherein R1 and Z are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of Formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of Formula (I).
