Synthesis and Evaluation of Artemisinin-Based Hybrid and Dimer Derivatives as Antimelanoma Agents

  • ACS Omega. 2019 Dec 27;5(1):243-251. doi: 10.1021/acsomega.9b02600.
Lorenzo Botta  1 ,  Silvia Filippi  1 ,  Bruno M Bizzarri  1 ,  Claudio Zippilli  1 ,  Roberta Meschini  1 ,  Rebecca Pogni  2 ,  Maria Camilla Baratto  2 ,  Luciano Villanova  3 ,  Raffaele Saladino  1
Affiliations
  • 1. Department of Ecological and Biological Sciences, University of Tuscia, via S. C. De Lellis 44, 01100, Viterbo, Italy.
  • 2. Department of Biotechnology, Chemistry and Pharmacy, University of Siena, via Aldo Moro 2, 53100 Siena, Italy.
  • 3. Lachifarma s.r.l., S.S.16 Zona Industriale, 73010, Zollino, Lecce, Italy.
PMID: 31956771 DOI: 10.1021/acsomega.9b02600
Abstract

A library of hybrid and dimer compounds based on the natural scaffold of artemisinin was synthesized. These derivatives were obtained by coupling of artemisinin derivatives, artesunate, and dihydroartemisinin with a panel of phytochemical compounds. The novel artemisinin-based hybrids and dimers were evaluated for their Anticancer activity on a Cervical Cancer cell line (HeLa) and on three complementary Metastatic Melanoma cancer cell lines (SK-MEL3, SK-MEL24, and RPMI-7951). Two hybrid compounds obtained by coupling of artesunate with eugenol and tyrosol, and one of the dimer compounds containing curcumin, emerged as the most active and cancer-selective derivatives.