909806-51-5Relevant articles and documents
A convenient one-pot synthesis of Indane-1,2,3-triones by oxidation of indan-1-ones with N-bromosuccinimide-dimethyl sulfoxide reagent
Tatsugi, Jiro,Izawa, Yasuji
, p. 859 - 864 (1998)
Indane 1,2,3-triones (2(a-f)) have been synthesized via brommation of indan-1-ones (1(a-f)), followed by oxidation of the resulting brominated indan-1-ones with dimethyl sulfoxide in one pot in good yields.
Discovery, Structure-Activity Relationship, and Binding Mode of an Imidazo[1,2-a]pyridine Series of Autotaxin Inhibitors
Joncour, Agnès,Desroy, Nicolas,Housseman, Christopher,Bock, Xavier,Bienvenu, Natacha,Cherel, La?titia,Labeguere, Virginie,Peixoto, Christophe,Annoot, Denis,Lepissier, Luce,Heiermann, J?rg,Hengeveld, Willem Jan,Pilzak, Gregor,Monjardet, Alain,Wakselman, Emanuelle,Roncoroni, Veronique,Le Tallec, Sandrine,Galien, René,David, Christelle,Vandervoort, Nele,Christophe, Thierry,Conrath, Katja,Jans, Mia,Wohlkonig, Alexandre,Soror, Sameh,Steyaert, Jan,Touitou, Robert,Fleury, Damien,Vercheval, Lionel,Mollat, Patrick,Triballeau, Nicolas,Van Der Aar, Ellen,Brys, Reginald,Heckmann, Bertrand
, p. 7371 - 7392 (2017/09/23)
Autotaxin (ATX) is a secreted enzyme playing a major role in the production of lysophosphatidic acid (LPA) in blood through hydrolysis of lysophosphatidyl choline (LPC). The ATX-LPA signaling axis arouses a high interest in the drug discovery industry as it has been implicated in several diseases including cancer, fibrotic diseases, and inflammation, among others. An imidazo[1,2-a]pyridine series of ATX inhibitors was identified out of a high-throughput screening (HTS). A cocrystal structure with one of these compounds and ATX revealed a novel binding mode with occupancy of the hydrophobic pocket and channel of ATX but no interaction with zinc ions of the catalytic site. Exploration of the structure-activity relationship led to compounds displaying high activity in biochemical and plasma assays, exemplified by compound 40. Compound 40 was also able to decrease the plasma LPA levels upon oral administration to rats.
