1268273-92-2Relevant academic research and scientific papers
Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif
Filipski, Kevin J.,Guzman-Perez, Angel,Bian, Jianwei,Perreault, Christian,Aspnes, Gary E.,Didiuk, Mary T.,Dow, Robert L.,Hank, Richard F.,Jones, Christopher S.,Maguire, Robert J.,Tu, Meihua,Zeng, Dongxiang,Liu, Shenping,Knafels, John D.,Litchfield, John,Atkinson, Karen,Derksen, David R.,Bourbonais, Francis,Gajiwala, Ketan S.,Hickey, Michael,Johnson, Theodore O.,Humphries, Paul S.,Pfefferkorn, Jeffrey A.
, p. 4571 - 4578 (2013/08/15)
Glucokinase activators are a class of experimental agents under investigation as a therapy for Type 2 diabetes mellitus. An X-ray crystal structure of a modestly potent agent revealed the potential to substitute the common heterocyclic amide donor-acceptor motif for a pyridone moiety. We have successfully demonstrated that both pyridone and pyrimidone heterocycles can be used as a potent donor-acceptor substituent. Several sub-micromolar analogs that possess the desired partial activator profile were synthesized and characterized. Unfortunately, the most potent activators suffered from sub-optimal pharmacokinetic properties. Nonetheless, these donor-acceptor motifs may find utility in other glucokinase activator series or beyond.
HEAT SHOCK PROTEIN BINDING COMPOUNDS, COMPOSITIONS, AND METHODS FOR MAKING AND USING SAME
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Page/Page column 173; 174, (2011/04/13)
The present subject matter relates to a compound represented by the general formula (I) or (I') or a pharmacologically acceptable salt thereof; pharmaceutical compositions containing at least one of these compounds; methods of making at least one of these compounds; methods of using at least one of these compounds for treating and/or preventing various cancers and/or proliferation disorders; methods of using at least one of these compounds for monitoring the effectiveness of an anticancer therapy against various cancers. In one embodiment, the subject matter relates to compounds that bind with a level of specificity to heat shock protein 70 (Hsp70). In another embodiment, the subject matter relates to compounds that bind with a level of specificity to inhibit both heat shock protein 70 (Hsp70) and heat shock cognate protein 70 (Hsc70).
