42465-54-3Relevant articles and documents
A Convenient Formal [4+2] Heterocylization Route to Bis(triflyl)tetrahydroquinolines
Lázaro-Milla, Carlos,Almendros, Pedro
supporting information, p. 13534 - 13538 (2021/08/13)
We report the sustainable and efficient synthesis of a new type of quinoline derivatives bearing one or two SO2CF3 groups. The protocol is metal-, catalyst- and irradiation-free, involves the use of readily available and stable precursors, and avoids the formation of side products. Also, the mild conditions of the process allow the tolerance of a wide range of functional groups.
Design, synthesis, and biological evaluation of 4-Methyl quinazoline derivatives as anticancer agents simultaneously targeting phosphoinositide 3-kinases and histone deacetylases
Zhang, Kehui,Lai, Fangfang,Lin, Songwen,Ji, Ming,Zhang, Jingbo,Zhang, Yan,Jin, Jing,Fu, Rong,Wu, Deyu,Tian, Hua,Xue, Nina,Sheng, Li,Zou, Xiaowen,Li, Yan,Chen, Xiaoguang,Xu, Heng
, p. 6992 - 7014 (2019/06/07)
Polypharmacology is a promising paradigm in modern drug discovery. Herein, we have discovered a series of novel PI3K and HDAC dual inhibitors in which the hydroxamic acid moiety as the zinc binding functional group was introduced to a quinazoline-based PI3K pharmacophore through an appropriate linker. Systematic structure-activity relationship studies resulted in lead compounds 23 and 36 that simultaneously inhibited PI3K and HDAC with nanomolar potencies and demonstrated favorable antiproliferative activities. Compounds 23 and 36 efficiently modulated the expression of p-AKT and Ac-H3, arrested the cell cycle, and induced apoptosis in HCT116 cancer cells. Following pharmacokinetic studies, 23 was further evaluated in HCT116 and HGC-27 xenograft models to show significant in vivo anticancer efficacies with tumor growth inhibitions of 45.8% (po, 150 mg/kg) and 62.6% (ip, 30 mg/kg), respectively. Overall, this work shows promise in discovering new anticancer therapeutics by the approach of simultaneously targeting PI3K and HDAC pathways with a single molecule.
QUINAZOLINE DERIVATIVES AS PDE10A ENZYME INHIBITORS
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, (2013/04/24)
This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The pr