1352881-82-3Relevant articles and documents
Efficient salt-induced kinase inhibitor and preparation method thereof
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, (2021/09/04)
The invention discloses an efficient salt-induced kinase inhibitor and a preparation method thereof, and the efficient salt-induced kinase inhibitor is characterized by comprising substances of a chemical formula in the invention. The salt-induced kinase inhibitor with excellent performance has high inhibitory activity for in-vitro experiments and also has high cell inhibitory activity.
Fragment-Based Drug Discovery of Potent Protein Kinase C Iota Inhibitors
Kwiatkowski, Jacek,Liu, Boping,Tee, Doris Hui Ying,Chen, Guoying,Ahmad, Nur Huda Binte,Wong, Yun Xuan,Poh, Zhi Ying,Ang, Shi Hua,Tan, Eldwin Sum Wai,Ong, Esther Hq,Nurul, Dinie,Poulsen, Anders,Pendharkar, Vishal,Sangthongpitag, Kanda,Lee, May Ann,Sepramaniam, Sugunavathi,Ho, Soo Yei,Cherian, Joseph,Hill, Jeffrey,Keller, Thomas H.,Hung, Alvin W.
, p. 4386 - 4396 (2018/05/31)
Protein kinase C iota (PKC-i) is an atypical kinase implicated in the promotion of different cancer types. A biochemical screen of a fragment library has identified several hits from which an azaindole-based scaffold was chosen for optimization. Driven by a structure-activity relationship and supported by molecular modeling, a weakly bound fragment was systematically grown into a potent and selective inhibitor against PKC-i.
Novel pyrazolo[1,5-a]pyridines as PI3K inhibitors: Variation of the central linker group
Kendall, Jackie D.,Marshall, Andrew J.,Giddens, Anna C.,Tsang, Kit Yee,Boyd, Maruta,Frederick, Raphael,Lill, Claire L.,Lee, Woo-Jeong,Kolekar, Sharada,Chao, Mindy,Malik, Alisha,Yu, Shuqiao,Chaussade, Claire,Buchanan, Christina M.,Rewcastle, Gordon W.,Baguley, Bruce C.,Flanagan, Jack U.,Denny, William A.,Shepherd, Peter R.
supporting information, p. 41 - 46 (2014/01/06)
As part of our investigation into the pyrazolo[1,5-a]pyridines as novel PI3K inhibitors, we report a range of analogues where the central linker portion of the molecule was varied while retaining the pyrazolo[1,5-a]pyridine and arylsulfonyl or arylcarbonyl groups. Isostere generating software BROOD was used to assist with producing ideas. The isoform selectivity of the compounds varied from pan-PI3K for compound 41 to p110α-selective for compound 58 or p110δ-selective for compound 57. The latter two compounds varied only in their sulphur oxidation state.