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Bis(1H-2-indolyl)methanones as a novel class of inhibitors of the platelet-derived growth factor receptor kinase

Mahboobi, Siavosh ; Teller, S. ; Pongratz, H. ; Hufsky, H. ; Sellmer, A. ; Botzki, Alexander ; Uecker, A. ; Beckers, T. ; Baasner, S. ; Schächtele, C. ; Überall, F. ; Kassack, M. U. ; Dove, Stefan ; Böhmer, F.-D.


The novel lead bis(1H-2-indolyl)methanone inhibits autophosphorylation of platelet-derived growth factor (PDGF) receptor tyrosine kinase in intact cells. Various substituents in the 5- or 6-position of one indole ring increase or preserve potency, whereas most modifications of the ring structures and of the methanone group as well as substitution at both indoles result in weak or no activity. ...


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