- Efficient salt-induced kinase inhibitor and preparation method thereof
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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.
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- METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION
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Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods that restore DNA binding affinity of p53 mutants. The compounds of the present disclosure can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.
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Paragraph 0235
(2022/01/06)
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- Fragment-Based Drug Discovery of Potent Protein Kinase C Iota Inhibitors
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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.
- 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.
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p. 4386 - 4396
(2018/05/31)
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- HETEROAROMATIC COMPOUNDS AS PI3 KINASE MODULATORS AND METHODS OF USE
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The present invention provides heteroaromatic derivatives and pharmaceutical acceptable salts and formulations thereof useful in modulating the protein kinase activity, especially phosphatidylinositol 3-kinases (PI3 kinases) and mTOR, and in modulating inter- and/or intra-cellular signaling activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
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- Novel pyrazolo[1,5-a]pyridines as PI3K inhibitors: Variation of the central linker group
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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.
- 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.
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supporting information
p. 41 - 46
(2014/01/06)
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