62136-38-3Relevant academic research and scientific papers
A pentacyclic aurora kinase inhibitor (AKI-001) with high in vivo potency and oral bioavailability
Rawson, Thomas E.,Rüth, Matthias,Blackwood, Elizabeth,Burdick, Dan,Corson, Laura,Dotson, Jenna,Drummond, Jason,Fields, Carter,Georges, Guy J.,Goller, Bernhard,Halladay, Jason,Hunsaker, Thomas,Kleinheinz, Tracy,Krell, Hans-Willi,Li, Jun,Liang, Jun,Limberg, Anja,McNutt, Angela,Moffat, John,Phillips, Gail,Ran, Yingqing,Safina, Brian,Ultsch, Mark,Walker, Leslie,Wiesmann, Christian,Zhang, Birong,Zhou, Aihe,Zhu, Bing-Yan,Rüger, Petra,Cochran, Andrea G.
scheme or table, p. 4465 - 4475 (2009/07/11)
Aurora kinase inhibitors have attracted a great deal of interest as a new class of antimitotic agents. We report a novel class of Aurora inhibitors based on a pentacyclic scaffold. A prototype pentacyclic inhibitor 32 (AKI-001) derived from two early lead
Synthesis and biological activity of a novel class of pyridazine analogues as non-competitive reversible inhibitors of protein tyrosine phosphatase 1B (PTP1B).
Liljebris, Charlotta,Martinsson, Jessica,Tedenborg, Lars,Williams, Meredith,Barker, Emma,Duffy, James E S,Nygren, Alf,James, Stephen
, p. 3197 - 3212 (2007/10/03)
A series of novel pyridazine analogues were prepared and the structure-activity relationship of their behavior as inhibitors of PTP1B was evaluated. Most of the analogues had potencies in the low micromolar range. The in vitro kinetics of this compound series demonstrated that they were reversible non-competitive binders. This indicates that there may exist another site in the enzyme through which enzyme activity can be inhibited, which is not a recognized interaction domain. Some of the analogues exhibited high selectivity for other PTPases, for example, compound 12 mp showed 20-fold selectivity for PTP1B (IC50=5.6 microM) versus both TCPTP and LAR (>100 microM, respectively). In contrast to many tyrosine phosphatase mimetic inhibitors, this compound class lacks negative charge and thus showed high permeability across cell membranes. Selective analogues in the series were analyzed in an in vitro cellular assay, which showed increased insulin-stimulated insulin receptor phosphorylation.
Tetracyclic compounds from cyclopent[b]indoles. Synthesis of isoxazolo[3′,4′:5,4]cyclopent[b]indoles
Sangeetha,Prasad, K.J. Rajendra
, p. 65 - 70 (2007/10/03)
Cyclopentan-1′,2′-dione-1′-arylhydrazones 3 obtained from the Japp-Klingemann reaction of diazotised aniline derivatives 1 and 2-hydroxymethylenecyclopentanone 2 on acid catalysed cyclization afforded cyclopent[b]indoles 4. These on mixed aldol condensati
