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ID: ALA1143906
Journal: Bioorg Med Chem Lett
Title: TIE-2/VEGF-R2 SAR and in vitro activity of C3-acyl dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole analogs.
Authors: Underiner TL, Ruggeri B, Aimone L, Albom M, Angeles T, Chang H, Hudkins RL, Hunter K, Josef K, Robinson C, Weinberg L, Yang S, Zulli A.
Abstract: Orally bioavailable, dual inhibitors of TIE-2/VEGF-R2 were identified by elaborating the C3/N13 SAR around a fused pyrrolodihydroindazolocarbazole scaffold. Analogs bearing a C3-thiophencarbonyl group were evaluated in enzymatic and cellular biochemical assays; two orally bioavailable analogs were further profiled in functional assays and found to inhibit microvessel growth in rat aortic explant cultures and inhibit Ang-1-stimulated chemotaxis of HUVECs.
CiteXplore: 18343109