765948-99-0Relevant articles and documents
METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION
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Paragraph 0295, (2022/01/06)
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.
COMPOUNDS AS TNIK, IKKEPSILON AND TBK1 INHIBITORS AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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Paragraph 0637; 0644; 0645, (2016/11/14)
Provided is a compound of formula (I) as a TNIK (Traf2- and NCK-interacting kinase), IKKε (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor; the compound according to the present invention effectively inhibits TNIK, IKKε and TBK1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, CNS cancer, colon cancer, non-small cell lung cancer, kidney cancer, prostate cancer, ovarian cancer, uterus cancer, stomach cancer, liver cancer, skin cancer, lung cancer, brain cancer, bladder cancer, esophageal cancer, pancreatic cancer, thyroid cancer, head and neck cancer, squamous cell carcinoma, osteosarcoma, B-cell or T-cell lymphoma, acute or chronic leukemia and multiple myeloma, but as a therapeutic agent for chronic inflammation.
Isoindolinone kinase inhibitors
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Page/Page column 11, (2010/02/10)
Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
Isoindolinone ureas: A novel class of KDR kinase inhibitors
Curtin, Michael L.,Frey, Robin R.,Heyman, H. Robin,Sarris, Kathy A.,Steinman, Douglas H.,Holmes, James H.,Bousquet, Peter F.,Cunha, George A.,Moskey, Maria D.,Ahmed, Asma A.,Pease, Lori J.,Glaser, Keith B.,Stewart, Kent D.,Davidsen, Steven K.,Michaelides, Michael R.
, p. 4505 - 4509 (2007/10/03)
A series of substituted isoindolinone ureas was prepared and evaluated for enzymatic and cellular inhibition of KDR kinase activity. Several of these analogs, such as 14c, are potent inhibitors of KDR both enzymatically (50nM) and cellularly (≤100nM). A 3D KDR/CDK2/MAP kinase overlay model with several structurally related tyrosine kinase inhibitors was used to predict the binding interactions of the isoindolinone ureas with the KDR active site.
ISOINDOLIN-1-ONE COMPOUNDS AS KINASE INHIBITORS
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Page 23, (2010/02/09)
Compounds having the formula, (I) are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds and compositions containing the compounds.