172734-33-7Relevant articles and documents
NHC-coordinated palladacycle catalyzed 1,2-addition of arylboronates to unactivated ketones
Akiyama, Ryo,Sugaya, Mariko,Shinozaki, Hiraku,Yamamoto, Tetsuya
, p. 1193 - 1201 (2019)
Palladium catalyzed intermolecular 1,2-addition of arylboronate to unactivated ketone was investigated. NHC-coordinated palladacycle 4c exhibited catalytic activity for the reactions and provided the corresponding tertiary alcohols and γ,γ-disubstituted γ-lactones in good to excellent yields.
Propafenone analogue with additional H-bond acceptor group shows increased inhibitory activity on P-glycoprotein
Cseke, Anna,Decker, Simon,Ecker, Gerhard F.,Jain, Sankalp,Schwarz, Theresa,Urban, Ernst,Vogl, Kerstin
, (2020/01/21)
P-glycoprotein (P-gp) is an ATP-dependent efflux pump that has a marked impact on the absorption, distribution, and excretion of therapeutic drugs. As P-gp inhibition can result in drug–drug interactions and altered drug bioavailability, identifying molec
Piperidine carbamate peptidomimetic inhibitors of the serine proteases HGFA, matriptase and hepsin
Damalanka, Vishnu C.,Wildman, Scott A.,Janetka, James W.
supporting information, p. 1646 - 1655 (2019/09/30)
Matriptase and hepsin are type II transmembrane serine proteases (TTSPs). Along with related S1 trypsin like serine protease HGFA (hepatocyte growth factor activator), their unregulated proteolytic activity has been associated with cancer including tumor progression and metastasis. These three proteases have two substrates in common, hepatocyte growth factor (HGF) and macrophage stimulating protein (MSP), the ligands for MET and recepteur d'origine nantais (RON) receptor tyrosine kinases. Mechanism-based tetrapeptide and benzamidine inhibitors of these proteases have been shown to block HGF/MET and MSP/RON cancer cell signaling. Herein, we have rationally designed a new class of peptidomimetic hybrid small molecule piperidine carbamate dipeptide inhibitors comparable in potency to much larger tetrapeptides. We have identified multiple compounds which have potent activity against matriptase and hepsin and with excellent selectivity over the off-target serine proteases factor Xa and thrombin.
