194473-04-6Relevant articles and documents
Method for preparing quinazolone and derivatives thereof by using chitosan-loaded copper catalyst
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Paragraph 0108-0114, (2021/05/12)
The invention discloses a method for preparing quinazolone and derivatives thereof by using a chitosan-loaded copper catalyst, which comprises the following steps of replacing residual gas in a reaction container with inert gas, adding a catalytic amount of copper ion-loaded chitosan catalyst, substituted 2-halogenated benzoic acid, substituted amidine hydrochloride, inorganic alkali and a mixed solvent into the reaction container, and heating for reaction, after the reaction time is 2-18 hours, extracting the product by using ethyl acetate, filtering and recovering the copper ion-loaded chitosan catalyst, concentrating the filtrate under reduced pressure, and purifying the product by column chromatography. The method has the advantages of low catalyst dosage, recoverability, easy separation after reaction, no metal residue, simple post-treatment, and suitableness for large-scale production.
Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases
Baska, Ferenc,Sipos, Anna,?rfi, Zoltán,Nemes, Zoltán,Dobos, Judit,Szántai-Kis, Csaba,Szabó, Eszter,Szénási, Gábor,Dézsi, László,Hamar, Péter,Cserepes, Mihály T.,Tóvári, József,Garamv?lgyi, Rita,Krekó, Marcell,?rfi, László
, (2019/10/16)
Aberrant activation of FMS-like tyrosine receptor kinase 3 (FLT3) is implicated in the pathogenesis of acute myeloid leukemia (AML) in 20–30% of patients. In this study we identified a highly selective (phenylethenyl)quinazoline compound family as novel potent inhibitors of the FLT3-ITD and FLT3-D835Y kinases. Their prominent effects were confirmed by biochemical and cellular proliferation assays followed by mice xenograft studies. Our modelling experiments and the chemical structures of the compounds predict the possibility of covalent inhibition. The most effective compounds triggered apoptosis in FLT3-ITD AML cells but had either weak or no effect in FLT3-independent leukemic and non-leukemic cell lines. Our results strongly suggest that our compounds may become therapeutics in relapsing and refractory AML disease harboring various ITD and tyrosine kinase domain mutations, by their ability to overcome drug resistance.
STYRYL QUINAZOLINE DERIVATIVES AS PHARMACEUTICALLY ACTIVE AGENTS
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Page/Page column 8, (2015/02/25)
The present invention relates to styryl quinazoline derivatives of the general formula (I) and pharmaceutically acceptable solvates, hydrates, salts, regioisomeric and polymorphic forms thereof as well as pharmaceutical compositions containing at least on