4946-08-1Relevant academic research and scientific papers
Dihydro quinazolinone derivative, as well as preparation method and application thereof
-
Paragraph 0127; 0128; 0129, (2018/07/30)
The invention relates to the technical field of medicines, in particular to a new dihydro quinazolinone derivative with the following chemical structure general formula and pharmaceutically acceptablesalts thereof, (the formula is shown in the description.), A pharmacological experiment shows that the derivative or the salt provided by the invention has higher inhibitory activity on KRAS-PDE delta protein interaction, and has higher anti-tumor activity in vitro. The invention also provides a preparation method of the derivative and the pharmaceutically acceptable salts thereof, and application to preparatioin of a KRAS-PDE delta inhibitor and an anti-tumor drug.
Discovery of Novel KRAS-PDEδ Inhibitors by Fragment-Based Drug Design
Chen, Long,Zhuang, Chunlin,Lu, Junjie,Jiang, Yan,Sheng, Chunquan
supporting information, p. 2604 - 2610 (2018/03/26)
Targeting KRAS-PDEδ protein-protein interactions with small molecules represents a promising opportunity for developing novel antitumor agents. However, current KRAS-PDEδ inhibitors are limited by poor cellular antitumor potency and the druggability of the target remains to be validated by new inhibitors. To tackle these challenges, herein, novel, highly potent KRAS-PDEδ inhibitors were identified by fragment-based drug design, providing promising lead compounds or chemical probes for investigating the biological functions and druggability of KRAS-PDEδ interaction.
Copper-catalyzed benzylic C(sp3)-H alkoxylation of heterocyclic compounds
Takemura, Noriaki,Kuninobu, Yoichiro,Kanai, Motomu
supporting information, p. 2528 - 2532 (2014/04/17)
We achieved intra- and intermolecular C(sp3)-H alkoxylation of benzylic positions of heteroaromatic compounds using CuBrn (n = 1, 2)/5,6-dimethylphenanthroline (or 4,7-dimethoxyphenanthroline) and ( tBuO)2 as a
NOVEL PYRAZOLE AND IMIDAZOLE DERIVATIVES USEFUL AS OREXIN ANTAGONISTS
-
Page/Page column 40, (2012/09/10)
The present invention relates to pyrazole and imidazole derivatives of formula (I) wherein U, V, L, X, Y, R1, (R2)n and (R3)m and ring A are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.
Synthesis of 1,2-disubstituted benzimidazoles by a Cu-catalyzed cascade aryl amination/condensation process
Zou, Benli,Yuan, Qiliang,Ma, Dawei
, p. 2598 - 2601 (2008/02/13)
(Chemical Equation Presented) Helpful neighbors: A wide range of 1,2-disubstituted benzimidazoles can be assembled from 2-haloanilides and primary amines by using a copper-catalyzed amination reaction promoted by an orthosubstituent effect of an NHCOR gro
