26759-52-4Relevant articles and documents
HETEROCYCLIC DERIVATIVES AND USE THEREOF
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Page/Page column 69, (2015/01/06)
A heterocyclic derivative represented by formula (I), or a pharmaceutically acceptable salt or a stereoisomer thereof, which has an inhibitory effect on the activation of STAT3 protein, and is useful for the prevention or treatment of diseases associated with the activation of STAT3 protein.
Synthesis and structure-activity relationships of benzothienothiazepinone inhibitors of protein kinase D
Bravo-Altamirano, Karla,George, Kara M.,Frantz, Marie-Celine,Lavalle, Courtney R.,Tandon, Manuj,Leimgruber, Stephanie,Sharlow, Elizabeth R.,Lazo, John S.,Wang, Q. Jane,Wipf, Peter
scheme or table, p. 154 - 159 (2011/04/15)
Protein kinase D (PKD) is a member of a novel family of serine/threonine kinases that regulate fundamental cellular processes. PKD is implicated in the pathogenesis of several diseases, including cancer. Progress in understanding the biological functions and therapeutic potential of PKD has been hampered by the lack of specific inhibitors. The benzoxoloazepinolone CID755673 was recently identified as the first potent and selective PKD inhibitor. The study of structure-activity relationships (SAR) of this lead compound led to further improvements in PKD1 potency. We describe herein the synthesis and biological evaluation of novel benzothienothiazepinone analogues. We achieved a 10-fold increase in the in vitro PKD1 inhibitory potency for the second generation lead kb-NB142-70 and accomplished a transition to an almost equally potent novel pyrimidine scaffold, while maintaining excellent target selectivity. These promising results will guide the design of pharmacological tools to dissect PKD function and pave the way for the development of potential anticancer agents.
