Bioorganic & Medicinal Chemistry Letters 28 (2018) 1001–1004 Contents lists available at ScienceDirect Bioorganic & Medicinal Chemistry Letters journal homepage: www.elsevier.com/locate/bmcl Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors a,⇑ b a a c Andrea Milelli , Chiara Marchetti , Eleonora Turrini , Elena Catanzaro , Roberta Mazzone , c a a b Daniela Tomaselli , Carmela Fimognari , Vincenzo Tumiatti , Anna Minarini Department for Life Quality Studies, Alma Mater Studiorum-University of Bologna, Corso d’Augusto 237, 47921 Rimini, Italy Department of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy Department of Drug Chemistry and Technologies, Sapienza University of Rome, P.le Aldo Moro 5, 00185 Roma, Italy article i nfo abstract Article history: Epigenetic modulators Histone deacetylases (HDACs) and Lysine demethylase (LSD1) are validated tar- Received 29 November 2017 gets for anticancer therapy. Both HDAC1/2 and LSD1 are found in association with the repressor protein Revised 15 February 2018 CoREST in a transcriptional co-repressor complex, which is responsible for gene silencing. Combined Accepted 16 February 2018 modulation of both targets results in a synergistic antiproliferative activity. In the present investigation, Available online 17 February 2018 we report about the design and synthesis
Bioorganic & Medicinal Chemistry Letters – Elsevier
Published: Apr 1, 2018
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