Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors

Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors 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 http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Bioorganic & Medicinal Chemistry Letters Elsevier

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Publisher
Elsevier
Copyright
Copyright © 2018 Elsevier Ltd
ISSN
0960-894x
D.O.I.
10.1016/j.bmcl.2018.02.034
Publisher site
See Article on Publisher Site

Abstract

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

Journal

Bioorganic & Medicinal Chemistry LettersElsevier

Published: Apr 1, 2018

References

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