2. Academic Validation
  3. New amidine-benzenesulfonamides as iNOS inhibitors for the therapy of the triple negative breast cancer

New amidine-benzenesulfonamides as iNOS inhibitors for the therapy of the triple negative breast cancer

  • Eur J Med Chem. 2023 Feb 15;248:115112. doi: 10.1016/j.ejmech.2023.115112.
M Dora Carrión 1,  Belén Rubio-Ruiz 2,  Francisco Franco-Montalban 1,  Pasquale Amoia 3,  Maria Chiara Zuccarini 4,  Chiara De Simone 4,  M Encarnación Camacho 5,  Rosa Amoroso 6,  Cristina Maccallini 3
Affiliations

Affiliations

  • 1 Department of Medicinal and Organic Chemistry, Faculty of Pharmacy, Campus Cartuja s/n, University of Granada, 18071, Granada, Spain.
  • 2 Department of Medicinal and Organic Chemistry, Faculty of Pharmacy, Campus Cartuja s/n, University of Granada, 18071, Granada, Spain; GENYO, Centre for Genomics and Oncological Research, Pfizer/University of Granada/Andalusian Regional Government, PTS Granada, Avda. Ilustración 114, 18016, Granada, Spain.
  • 3 Department of Pharmacy, University "G. d'Annunzio" of Chieti-Pescara, Via dei Vestini 31, 66100, Chieti, Italy.
  • 4 Department of Medical, Oral and Biotechnological Sciences, University "G. d'Annunzio" of Chieti-Pescara, Via dei Vestini 31, 66100, Chieti, Italy.
  • 5 Department of Medicinal and Organic Chemistry, Faculty of Pharmacy, Campus Cartuja s/n, University of Granada, 18071, Granada, Spain. Electronic address: ecamacho@ugr.es.
  • 6 Department of Pharmacy, University "G. d'Annunzio" of Chieti-Pescara, Via dei Vestini 31, 66100, Chieti, Italy. Electronic address: rosa.amoroso@unich.it.
PMID: 36641860 DOI: 10.1016/j.ejmech.2023.115112
Abstract

Triple negative breast Cancer (TNBC) is a specific breast Cancer subtype, and poor prognosis is associated to this tumour when it is in the metastatic form. The overexpression of the inducible Nitric Oxide Synthase (iNOS) is considered a predictor of poor outcome in TNBC patients, and this Enzyme is reported as a valuable molecular target to compromise TNBC progression. In this work, new amidines containing a benzenesulfonamide group were designed and synthesized as selective iNOS inhibitors. An in vitro biological evaluation was performed to assess compounds activity against both the inducible and constitutive NOSs. The most interesting compounds 1b and 2b were evaluated on MDA-MB-231 cells as antiproliferative agents, and 1b capability to counteract cell migration was also studied. Finally, an in-depth docking study was performed to shed light on the observed potency and selectivity of action of the most promising compounds.

Keywords

Amidines; Anticancer; Benzensulfonamides; Docking; Nitric oxide synthase inhibitors; Synthesis.

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