99847-13-9Relevant articles and documents
Copper-catalyzed oxidative decarboxylative C-H arylation of benzoxazoles with 2-nitrobenzoic acids
Chen, Lijun,Ju, Lin,Bustin, Katelyn A.,Hoover, Jessica M.
, p. 15059 - 15062 (2015/10/12)
A copper-catalyzed oxidative decarboxylative coupling of benzoxazoles with 2-nitrobenzoic acids was developed. This methodology favors electron-rich benzoxazoles and electron-deficient benzoic acids and enables the preparation of a variety of arylated benzoxazoles in good yields. The trends in product yields suggest a delicate balance between the decarboxylation and C-H arylation steps.
Potent galloyl-based selective modulators targeting multidrug resistance associated protein 1 and P-glycoprotein
Pellicani, Raffaella Zoe,Stefanachi, Angela,Niso, Mauro,Carotti, Angelo,Leonetti, Francesco,Nicolotti, Orazio,Perrone, Roberto,Berardi, Francesco,Cellamare, Saverio,Colabufo, Nicola Antonio
supporting information; experimental part, p. 424 - 436 (2012/03/10)
The multifactorial nature of chemotherapy failure in controlling cancer is often associated with the occurrence of multidrug resistance (MDR), a phenomenon likely related to the increased expression of members of the ATP binding cassette (ABC) transporter superfamily. In this respect, the most extensively characterized MDR transporters include ABCB1 (also known as MDR1 or P-glycoprotein) and ABCC1 (also known as MRP1) whose inhibition remains a priority to circumvent drug resistance. Herein, we report how the simple galloyl benzamide scaffold can be easily and properly decorated for the preparation of either MRP1 or P-gp highly selective inhibitors. In particular, some gallamides and pyrogallol-1-monomethyl ethers showed remarkable affinity and selectivity toward MRP1. On the other hand, trimethyl ether galloyl anilides, with few exceptions, exhibited moderate to very high and selective P-gp inhibition.
Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849
Witty, David R.,Bateson, John,Hervieu, Guillaume J.,Al-Barazanji, Kamal,Jeffrey, Phillip,Hamprecht, Dieter,Haynes, Andrea,Johnson, Christopher N.,Muir, Alison I.,O'Hanlon, Peter J.,Stemp, Geoffrey,Stevens, Alex J.,Thewlis, Kevin,Winborn, Kim Y.
, p. 4872 - 4878 (2007/10/03)
A strategy of systematically targeting more rigid analogues of the known MCH R1 receptor antagonist, SB-568849, serendipitously uncovered a binding mode accessible to N-aryl-phthalimide ligands. Optimisation to improve the stability of this compound class led to the discovery of novel N-aryl-quinazolinones, benzotriazinones and thienopyrimidinones as selective ligands with good affinity for human melanin-concentrating hormone receptor 1.