Synthesis and Antiproliferative Activity of Triazoles Based on 2-Azabicycloalkanes

A library of 21 novel chiral 1,2,3-triazole-based 2-azabicycloalkane conjugates was designed and synthesized using the copper(I)-catalyzed click reaction. The obtained hybrids were assessed for their antiproliferative potency against three selected human cancer cell lines: Hs294T (melanoma), MIA PaC...

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Autores principales: Steppeler, Franz, Kłopotowska, Dagmara, Wietrzyk, Joanna, Wojaczyńska, Elżbieta
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Communication
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8072719/
https://www.ncbi.nlm.nih.gov/pubmed/33919613
http://dx.doi.org/10.3390/ma14082039
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author Steppeler, Franz
Kłopotowska, Dagmara
Wietrzyk, Joanna
Wojaczyńska, Elżbieta
author_facet Steppeler, Franz
Kłopotowska, Dagmara
Wietrzyk, Joanna
Wojaczyńska, Elżbieta
author_sort Steppeler, Franz
collection PubMed
description A library of 21 novel chiral 1,2,3-triazole-based 2-azabicycloalkane conjugates was designed and synthesized using the copper(I)-catalyzed click reaction. The obtained hybrids were assessed for their antiproliferative potency against three selected human cancer cell lines: Hs294T (melanoma), MIA PaCa-2 (pancreas tumor) and NCI-H1581 (lung tumor). The majority of the synthesized compounds demonstrated moderate to potent activity, and some of them appeared more selective than cisplatin, with selectivity index exceeding 9.
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spelling pubmed-80727192021-04-27 Synthesis and Antiproliferative Activity of Triazoles Based on 2-Azabicycloalkanes Steppeler, Franz Kłopotowska, Dagmara Wietrzyk, Joanna Wojaczyńska, Elżbieta Materials (Basel) Communication A library of 21 novel chiral 1,2,3-triazole-based 2-azabicycloalkane conjugates was designed and synthesized using the copper(I)-catalyzed click reaction. The obtained hybrids were assessed for their antiproliferative potency against three selected human cancer cell lines: Hs294T (melanoma), MIA PaCa-2 (pancreas tumor) and NCI-H1581 (lung tumor). The majority of the synthesized compounds demonstrated moderate to potent activity, and some of them appeared more selective than cisplatin, with selectivity index exceeding 9. MDPI 2021-04-18 /pmc/articles/PMC8072719/ /pubmed/33919613 http://dx.doi.org/10.3390/ma14082039 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Communication
Steppeler, Franz
Kłopotowska, Dagmara
Wietrzyk, Joanna
Wojaczyńska, Elżbieta
Synthesis and Antiproliferative Activity of Triazoles Based on 2-Azabicycloalkanes
title Synthesis and Antiproliferative Activity of Triazoles Based on 2-Azabicycloalkanes
title_full Synthesis and Antiproliferative Activity of Triazoles Based on 2-Azabicycloalkanes
title_fullStr Synthesis and Antiproliferative Activity of Triazoles Based on 2-Azabicycloalkanes
title_full_unstemmed Synthesis and Antiproliferative Activity of Triazoles Based on 2-Azabicycloalkanes
title_short Synthesis and Antiproliferative Activity of Triazoles Based on 2-Azabicycloalkanes
title_sort synthesis and antiproliferative activity of triazoles based on 2-azabicycloalkanes
topic Communication
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8072719/
https://www.ncbi.nlm.nih.gov/pubmed/33919613
http://dx.doi.org/10.3390/ma14082039
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AT wojaczynskaelzbieta synthesisandantiproliferativeactivityoftriazolesbasedon2azabicycloalkanes

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