104612-36-4Relevant articles and documents
Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ
Liu, Linyi,Li, Xinyu,Cheng, Yu,Wang, Lianjian,Yang, Huizhu,Li, Jiurong,He, Siying,shuangjie Wu,Yin, Qianqian,Xiang, Hua
, p. 304 - 316 (2019)
BTK and PI3Kδ play crucial roles in the progression of leukemia, and studies confirmed that the dual inhibition against BTK and PI3Kδ could provide superior anticancer agents to single targeted therapies. Herein, a new series of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives were optimized based on a BTK/PI3Kδ inhibitor 2 designed by our group. Biological studies clarified that compound 6f exhibited the most potent inhibitory activity (BTK: IC50 = 74 nM; PI3Kδ: IC50 = 170 nM) and better selectivity than 2. Moreover, 6f significantly inhibited the proliferation of Raji and Ramos cells with IC50 values of 2.1 μM and 2.65 μM respectively by blocking BTK and PI3K signaling pathways. In brief, 6f possessed of the potency for further optimization as an anti-leukemic drug by inhibiting BTK and PI3Kδ kinase.
NOVEL COMPOUNDS FOR THE TREATMENT OF HEPATITIS C
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Page/Page column 31, (2016/09/26)
The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
HETEROCYCLIC UREA DERIVATIVES AND METHODS OF USE THEREOF
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Page/Page column 112, (2010/12/26)
Compounds of formula (IA) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.