516465-80-8Relevant articles and documents
Design, synthesis and biological evaluation of isoxazole-based CK1 inhibitors modified with chiral pyrrolidine scaffolds
Luxenburger, Andreas,Schmidt, Dorian,Ianes, Chiara,Pichlo, Christian,Krüger, Marc,von Drathen, Thorsten,Brunstein, Elena,Gainsford, Graeme J.,Baumann, Ulrich,Knippschild, Uwe,Peifer, Christian
, (2019/03/19)
In this study, we report on the modification of a 3,4-diaryl-isoxazole-based CK1 inhibitor with chiral pyrrolidine scaffolds to develop potent and selective CK1 inhibitors. The pharmacophore of the lead structure was extended towards the ribose pocket of
A Modular Synthesis of the Lamellarins: Total Synthesis of Lamellarin G Trimethyl Ether
Handy, Scott T.,Zhang, Yanan,Bregman, Howard
, p. 2362 - 2366 (2007/10/03)
A modular synthesis of the lamellarin family of natural products has been developed that is based on the application of three iterative halogenation/cross-coupling reaction sequences. The ability to halogenate the pyrrole core in a regioselective fashion, even in the presence of highly electron-rich aryl substituents, has been established. The compatibility of Suzuki coupling conditions with free alcohols and phenols in the boronic acids has been employed to reduce the number of protection/deprotection steps. Indeed, the presence of a free phenol on boronic acid 3 has been determined to be critical for the successful final coupling in route to lamellarin G trimethyl ether, since protected versions fail to undergo coupling.