443331-84-8Relevant academic research and scientific papers
Integrin receptors antagonists
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Page/Page column 93, (2010/11/23)
The invention relates to novel compounds which bind to integrin receptors, and to the preparation thereof and the use thereof as drugs.
Synthesis and SAR of N-substituted dibenzazepinone derivatives as novel potent and selective αVβ3 antagonists
Kling, Andreas,Backfisch, Gisela,Delzer, Juergen,Geneste, Herve,Graef, Claudia,Holzenkamp, Uta,Hornberger, Wilfried,Lange, Udo E.W,Lauterbach, Arnulf,Mack, Helmut,Seitz, Werner,Subkowski, Thomas
, p. 441 - 446 (2007/10/03)
Synthesis and SARs of new integrin αVβ3 antagonists based on an N-substituted dibenzazepinone scaffold are described. Variation of spacer and guanidine mimetic led to potent compounds exhibiting an IC50 towards αVβ3 in the nanomolar range, high selectivity versus integrin αIIbβ3 and efficacy in functional cellular assays.
