911301-34-3Relevant articles and documents
Thermal and photochemical annulation of vinyl azides to 2-aminoimidazoles
Man, Lucas,Copley, Royston C.B.,Handlon, Anthony L.
supporting information, p. 6566 - 6569 (2019/07/16)
2-Aminoimidazoles represent useful synthons for incorporation into medicinal compounds. They provide hydrogen bonding loci, water solubilizing properties and convenient handles for further synthetic elaboration. The rapid and facile generation of diverse
Indol-2-yl ethanones as novel indoleamine 2,3-dioxygenase (IDO) inhibitors
Dolusic, Eduard,Larrieu, Pierre,Blanc, Sebastien,Sapunaric, Frederic,Norberg, Bernadette,Moineaux, Laurence,Colette, Delphine,Stroobant, Vincent,Pilotte, Luc,Colau, Didier,Ferain, Thierry,Fraser, Graeme,Galeni, Moreno,Frre, Jean-Marie,Masereel, Bernard,Van Den Eynde, Benoit,Wouters, Johan,Frederick, Raphael
experimental part, p. 1550 - 1561 (2011/03/22)
Indoleamine 2,3-dioxygenase (IDO) is a heme dioxygenase which has been shown to be involved in the pathological immune escape of diseases such as cancer. The synthesis and structure-activity relationships (SAR) of a novel series of IDO inhibitors based on the indol-2-yl ethanone scaffold is described. In vitro and in vivo biological activities have been evaluated, leading to compounds with IC50 values in the micromolar range in both tests. Introduction of small substituents in the 5- and 6-positions of the indole ring, indole N-methylation and variations of the aromatic side chain are all well tolerated. An iron coordinating group on the linker is a prerequisite for biological activity, thus corroborating the virtual screening results.
