63286-28-2Relevant academic research and scientific papers
HERBICIDAL COMPOUNDS
-
Page/Page column 101, (2021/04/02)
Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a 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.
tele-Substitution Reactions in the Synthesis of a Promising Class of 1,2,4-Triazolo[4,3- a]pyrazine-Based Antimalarials
Korsik, Marat,Tse, Edwin G.,Smith, David G.,Lewis, William,Rutledge, Peter J.,Todd, Matthew H.
, p. 13438 - 13452 (2020/12/15)
We have discovered and studied a tele-substitution reaction in a biologically important heterocyclic ring system. Conditions that favor the tele-substitution pathway were identified: the use of increased equivalents of the nucleophile or decreased equivalents of base or the use of softer nucleophiles, less polar solvents, and larger halogens on the electrophile. Using results from X-ray crystallographic and isotope labeling experiments, a mechanism for this unusual transformation is proposed. We focused on this triazolopyrazine as it is the core structure of the in vivo active antiplasmodium compounds of Series 4 of the Open Source Malaria consortium.
PYRIDAZINIUM COMPOUNDS FOR USE IN CONTROLLING UNWANTED PLANT GROWTH
-
Page/Page column 57, (2020/08/22)
Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as pesticides, especially as herbicides.
An original class of small sized molecules as versatile fluorescent probes for cellular imaging
Sirbu, Doina,Diharce, Julien,Martini?, Ivana,Chopin, Nicolas,Eliseeva, Svetlana V.,Guillaumet, Gérald,Petoud, Stéphane,Bonnet, Pascal,Suzenet, Franck
supporting information, p. 7776 - 7779 (2019/07/08)
An unusual class, compact in size, of fluorescent probes based on pyridazino-1,3a,6a-triazapentalene scaffolds exhibits promising fluorescent properties (quantum yield values up to 73%, large Stokes shifts, emission wavelengths located in the green-yellow
COMBINATION TREATMENT OF ACUTE MYELOID LEUKEMIA
-
Page/Page column 20; 34, (2019/08/12)
The present invention relates to the use of volasertib, or a pharmaceutically acceptable salt thereof or a hydrate thereof, in combination with a BET inhibitor, or a pharmaceutically acceptable salt thereof or a hydrate thereof for treating patients suffering from acute myeloid leukemia (AML).
Preparation and application of triazole heterocyclic compound containing heteroaryl amide structure
-
Paragraph 0085-0088, (2019/11/14)
The invention discloses a triazole heterocyclic compound containing a heteroaryl amide structure, a geometrical isomer of triazole heterocyclic compound containing the heteroaryl amide structure and pharmacologically acceptable salt, hydrate, solvate or p
Triazolo pyrazine compound containing heteroaryl substituted pyridazinone structure, and preparation method and applications thereof
-
Paragraph 0076; 0078-0079, (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
Compound as potassium channel modulator
-
Paragraph 0775; 0777; 0778; 0779, (2018/07/30)
The invention relates to a compound as a potassium channel modulator, which is a compound of a formula (I) or a pharmaceutically acceptable salt thereof. The compound or the pharmaceutically acceptable salt thereof is effective for curing and preventing diseases and symptoms influenced by the activity of potassium ion channels.
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.
