- 2-thioxothiazolidin-4-one analogs as pan-pim kinase inhibitors
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Proviral integration site for Moloney murine leukemia virus (PIM) kinases are proto-oncogenic kinases involved in the regulation of several cellular processes. PIM kinases are promising targets for new drug development because they play a major role in many cancer-specific pathways, such as survival, apoptosis, proliferation, cell cycle regulation, and migration. Here, 2-thioxothiazolidin-4-one derivatives were synthesized and evaluated as potent pan-PIM kinase inhibitors. Optimized compounds showed single-digit nanomolar IC50 values against all three PIM kinases with high selectivity over 14 other kinases. Compound 17 inhibited the growth of Molm-16 cell lines (EC50 = 14 nM) and modulated the expression of pBAD and p4EBP1 in a dose-dependent manner.
- Yun, Yanghwan,Hong, Victor Sukbong,Jeong, Seungik,Choo, Hyeonseong,Kim, Shin,Lee, Jinho
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p. 854 - 861
(2021/09/06)
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- PYRAZOLE PYRAZINE AMINE COMPOUNDS AS KINASE INHIBITORS, COMPOSITIONS THEREOF AND METHODS OF TREATMENT THEREWITH
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Provided herein are Pyrazole Pyrazine Amine Compounds having the following structure:Formula (I). Wherein Q and R1-R3 are as defined herein, compositions comprising an effective amount of a Pyrazole Pyrazine Amine Compound and methods for treating or preventing inflammatory conditions, immunological conditions, cancer, neurodegenerative diseases, age-related diseases, cardiovascular diseases and metabolic conditions, or conditions treatable or preventable by inhibition of an IKK, or an IKK pathway, comprising administering an effective amount of a Pyrazole Pyrazine Amine Compound to a patient in need thereof.
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Page/Page column 96
(2009/09/04)
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- PYRAZINE DERIVATIVES AND THEIR USE AS POTASSIUM CHANNEL MODULATORS
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This invention relates to novel pyrazine derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with t
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Page/Page column 22
(2009/04/25)
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