2. Academic Validation
  3. Coumarin derivatives as potential antitumor agents: Growth inhibition, apoptosis induction and multidrug resistance reverting activity

Coumarin derivatives as potential antitumor agents: Growth inhibition, apoptosis induction and multidrug resistance reverting activity

  • Eur J Med Chem. 2017 Feb 15:127:577-585. doi: 10.1016/j.ejmech.2017.01.020.
Alessandra Bisi 1,  Concettina Cappadone 2,  Angela Rampa 3,  Giovanna Farruggia 4,  Azzurra Sargenti 5,  Federica Belluti 3,  Rita M C Di Martino 3,  Emil Malucelli 5,  Alessia Meluzzi 5,  Stefano Iotti 4,  Silvia Gobbi 3
Affiliations

Affiliations

  • 1 Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via Belmeloro, 6, 40126 Italy. Electronic address: alessandra.bisi@unibo.it.
  • 2 Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via S. Donato, 19/2, 40127 Bologna, Italy. Electronic address: concettina.cappadone@unibo.it.
  • 3 Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via Belmeloro, 6, 40126 Italy.
  • 4 Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via S. Donato, 19/2, 40127 Bologna, Italy; National Institute of Biostructures and Biosystems, Via delle Medaglie D'oro, 305, 00136 Roma, Italy.
  • 5 Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via S. Donato, 19/2, 40127 Bologna, Italy.
PMID: 28109950 DOI: 10.1016/j.ejmech.2017.01.020
Abstract

A small library of Coumarins, carrying butynyl-amino chains, was synthesized continuing our studies in the field of MDR reverting ageEnts and in order to obtain multipotent agents to combat malignancies. In particular, the reported Anticancer and chemopreventive natural product 7-isopentenyloxycoumarin was linked to different terminal amines, selected on the basis of our previously reported results. The Anticancer behaviour and the MDR reverting ability of the new compounds were evaluated on human colon Cancer cells, particularly prone to develop the MDR phenotype. Some of the new derivatives showed promising effects, directly acting as cytotoxic compounds and/or counteracting MDR phenomenon. Compound 1e emerged as the most interesting of this series, showing a multipotent biological profile and suggesting that conjugation of an appropriate coumarin core with a properly selected butynyl-amino chain allows to obtain novel hybrid molecules endowed with improved in vitro antitumor activity.

Keywords

Anticancer; Chemosensitizers; Coumarin; MDR modulators; P-glycoprotein.

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