- Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases
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Novel substituted benzylidene-1,3-thiazolidine-2,4-diones (TZDs) have been identified as potent and highly selective inhibitors of the PIM kinases. The synthesis and SAR of these compounds are described, along with X-ray crystallographic, anti-proliferati
- Dakin, Les A.,Block, Michael H.,Chen, Huawei,Code, Erin,Dowling, James E.,Feng, Xiaomei,Ferguson, Andrew D.,Green, Isabelle,Hird, Alexander W.,Howard, Tina,Keeton, Erika K.,Lamb, Michelle L.,Lyne, Paul D.,Pollard, Hannah,Read, Jon,Wu, Allan J.,Zhang, Tao,Zheng, Xiaolan
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p. 4599 - 4604
(2012/08/07)
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- CHEMICAL COMPOUNDS 251
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The invention relates to chemical compounds of formula (I), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of PIM-1 and/or PIM-2, and/or PIM-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of PIM kinase related conditions and diseases, preferably cancer.
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Page/Page column 117
(2011/10/02)
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