Journal
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
Volume 121, Issue -, Pages 77-88Publisher
ELSEVIER
DOI: 10.1016/j.ijbiomac.2018.09.153
Keywords
Benzofuran; Nucleic acid-interaction; Prostate cancer; Antiproliferative; Telomeric DNA
Funding
- University of Naples Federico II [000005 ALTRI_DR_409_2017_Rec_Ateneo_prof MARASCO]
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Four 4-nitrophenyl-functionalized benzofuran (BF1, BF2) and benzodifuran (BDF1, BDF2) compounds were synthesized by a convenient route based on the Craven reaction. All the compounds underwent a detailed chemical physical characterization to evaluate their structural, thermal and optical properties. An investigation on the therapeutic potential of the reported compounds was performed by analyzing their antiproliferative activity on prostatic tumour cells (PC-3). In both classes of compounds, anticancer potential is in direct correlation with the lipophilicity. From our study it emerged that antiproliferative activity was higher for benzofuran derivatives as compared to benzodifuran systems. Moreover, we report a mechanistic study relative to the most promising molecule, i.e. the apolar benzofuran BF1, that relates the antiproliferative properties found in our investigation to its ability to bind telomeric DNA (proven by CD and fluorescence techniques on tel(22) G4 DNA), and highlights its unexpected impact on cell cycle progression. (C) 2018 Elsevier B.V. All rights reserved.
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