885270-23-5Relevant articles and documents
General Ser/Thr Kinases Pharmacophore Approach for Selective Kinase Inhibitors Search as Exemplified by Design of Potent and Selective Aurora A Inhibitors
Vasilevich, Natalya I.,Aksenova, Elena A.,Kazyulkin, Denis N.,Afanasyev, Ilya I.
, p. 54 - 65 (2016/07/09)
A general pharmachophore model for various types of Ser/Thr kinases was developed. Search for the molecules fitting to this pharmacophore among ASINEX proprietary library revealed a number of compounds, which were tested and appeared to possess some activity against several Ser/Thr kinases such as Aurora A, Aurora B and Haspin. The possibility of performing the fine-tuning of the general Ser/Thr pharmacophore to desired types of kinase to get active and selective inhibitors was exemplified by Aurora A kinase. As a result, several hits in 3–5?nm range of activity against Aurora A kinase with rather good selectivity and ADME properties were obtained.
NOVEL KINASE INHIBITORS
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Paragraph 0217; 0218, (2014/05/07)
The present invention provides derivatives of thiazolylamino-substituted heterocycles. These compounds are inhibitors of kinases, including compounds that show antiproliferative activity against cells, including against tumor cells, and are useful in the treatment of diseases including cancer.
P70 S6 KINASE INHIBITORS
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Page/Page column 24-25, (2009/01/20)
The present invention provides p70 S6 kinase inhibitors of the formula: pharmaceutical formulations comprising them, and methods for their use.