5101-01-9Relevant academic research and scientific papers
Convergent synthesis of fully functionalized ringC C allocolchicinoids. Benzannulation approach
Vorogushin, Andrei V.,Wulff, William D.,Hansen, Hans-JUrgen
, p. 2641 - 2644 (2001)
(Equation presented) A novel convergent approach to fully functionalized ring C allocolchicinoids is developed which is based on the benzannulation reaction of Fischer carbene complexes with alkynes. The efficacy of this strategy was established with the
Rational design of novel, potent small molecule pan-selectin antagonists
Kranich, Remo,Busemann, Anke S.,Bock, Daniel,Schroeter-Maas, Sabine,Beyer, Diana,Heinemann, Bo,Meyer, Michael,Schierhorn, Katrin,Zahlten, Rainer,Wolff, Gerhard,Aydt, Ewald M.
, p. 1101 - 1115 (2007/10/03)
This report describes the first results of a rational hit-finding strategy to design novel small molecule antiinflammatory drugs targeting selectins, a family of three cellular adhesion molecules. Based on recent progress in understanding of molecular interaction between selectins and their natural ligands as well as progress in clinical development of synthetic antagonists like 1 (bimosiamose, TBC1269), this study was initiated to discover small molecule selectin antagonists with improved pharmacological properties. Considering 1 as template structure, a ligand-based approach followed by focused chemical synthesis has been applied to yield novel synthetic small molecules (MWr 500) with a trihydroxybenzene motif, bearing neither peptidic nor glycosidic components, with nanomolar in vitro activity. Biological evaluation involves two kinds of in vitro assays, a static molecular binding assay, and a dynamic HL-60 cell attachment assay. As compared to controls, the novel compounds showed improved biological in vitro activity both under static and dynamic conditions.
An approach to the biomimetic synthesis of aryltetralin lignans
Pelter, Andrew,Ward, Robert S.,Rao, Ramohan R.
, p. 2933 - 2938 (2007/10/02)
The BF3 catalysed cyclisation of 3-arylpropyl substituted quinone-methide ketals affords a mild, biomimetic route to aryltetralins. 1H- and 13C-NMR spectra of the products are reported.
