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ID: ALA1136337
Journal: Bioorg Med Chem Lett
Title: Studies on cyclin-dependent kinase inhibitors: indolo-[2,3-a]pyrrolo[3,4-c]carbazoles versus bis-indolylmaleimides.
Authors: Sanchez-Martinez C, Shih C, Zhu G, Li T, Brooks HB, Patel BK, Schultz RM, DeHahn TB, Spencer CD, Watkins SA, Ogg CA, Considine E, Dempsey JA, Zhang F.
Abstract: A series of indolo[2,3-a]pyrrolo[3,4-c]carbazoles and their bis-indolylmaleimides precursors have been prepared in order to compare their activity as D1-CDK4 inhibitors. Both enzymatic and antiproliferative assays have shown that the structurally more constrained indolo[2,3-a]pyrrolo[3,4-c]carbazoles are consistently more active (8-42-fold) in head-to-head comparison with their bis-indolylmaleimides counterparts. Cell-cycle analysis using flow cytometry have also shown that the indolocarbazoles are selective G1 blockers while the bis-indolylmaleimides arrest cells in the G2/M phase.
CiteXplore: 14552792