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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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Detalles Bibliográficos
Autores principales: Steppeler, Franz, Kłopotowska, Dagmara, Wietrzyk, Joanna, Wojaczyńska, Elżbieta
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
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
Descripción
Sumario: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.