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

[Image: see text] 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 hybr...

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Autores principales: Botta, Lorenzo, Filippi, Silvia, Bizzarri, Bruno M., Zippilli, Claudio, Meschini, Roberta, Pogni, Rebecca, Baratto, Maria Camilla, Villanova, Luciano, Saladino, Raffaele
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2019
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6964273/
https://www.ncbi.nlm.nih.gov/pubmed/31956771
http://dx.doi.org/10.1021/acsomega.9b02600
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author Botta, Lorenzo
Filippi, Silvia
Bizzarri, Bruno M.
Zippilli, Claudio
Meschini, Roberta
Pogni, Rebecca
Baratto, Maria Camilla
Villanova, Luciano
Saladino, Raffaele
author_facet Botta, Lorenzo
Filippi, Silvia
Bizzarri, Bruno M.
Zippilli, Claudio
Meschini, Roberta
Pogni, Rebecca
Baratto, Maria Camilla
Villanova, Luciano
Saladino, Raffaele
author_sort Botta, Lorenzo
collection PubMed
description [Image: see text] 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.
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spelling pubmed-69642732020-01-17 Synthesis and Evaluation of Artemisinin-Based Hybrid and Dimer Derivatives as Antimelanoma Agents Botta, Lorenzo Filippi, Silvia Bizzarri, Bruno M. Zippilli, Claudio Meschini, Roberta Pogni, Rebecca Baratto, Maria Camilla Villanova, Luciano Saladino, Raffaele ACS Omega [Image: see text] 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. American Chemical Society 2019-12-27 /pmc/articles/PMC6964273/ /pubmed/31956771 http://dx.doi.org/10.1021/acsomega.9b02600 Text en Copyright © 2019 American Chemical Society This is an open access article published under an ACS AuthorChoice License (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html) , which permits copying and redistribution of the article or any adaptations for non-commercial purposes.
spellingShingle Botta, Lorenzo
Filippi, Silvia
Bizzarri, Bruno M.
Zippilli, Claudio
Meschini, Roberta
Pogni, Rebecca
Baratto, Maria Camilla
Villanova, Luciano
Saladino, Raffaele
Synthesis and Evaluation of Artemisinin-Based Hybrid and Dimer Derivatives as Antimelanoma Agents
title Synthesis and Evaluation of Artemisinin-Based Hybrid and Dimer Derivatives as Antimelanoma Agents
title_full Synthesis and Evaluation of Artemisinin-Based Hybrid and Dimer Derivatives as Antimelanoma Agents
title_fullStr Synthesis and Evaluation of Artemisinin-Based Hybrid and Dimer Derivatives as Antimelanoma Agents
title_full_unstemmed Synthesis and Evaluation of Artemisinin-Based Hybrid and Dimer Derivatives as Antimelanoma Agents
title_short Synthesis and Evaluation of Artemisinin-Based Hybrid and Dimer Derivatives as Antimelanoma Agents
title_sort synthesis and evaluation of artemisinin-based hybrid and dimer derivatives as antimelanoma agents
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6964273/
https://www.ncbi.nlm.nih.gov/pubmed/31956771
http://dx.doi.org/10.1021/acsomega.9b02600
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