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. 2021 Apr 18;14(8):2039.
doi: 10.3390/ma14082039.

Synthesis and Antiproliferative Activity of Triazoles Based on 2-Azabicycloalkanes

Franz Steppeler  1 , Dagmara Kłopotowska  2 , Joanna Wietrzyk  2 , Elżbieta Wojaczyńska  1
Affiliations

Synthesis and Antiproliferative Activity of Triazoles Based on 2-Azabicycloalkanes

Franz Steppeler et al. Materials (Basel). .

Abstract

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.

Keywords: 2-azabicycloalkanes; CuAAC; antiproliferative activity; cancer; triazoles.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Selected biologically active compounds bearing triazole moieties.
Scheme 1
Scheme 1
Synthesis of mono-, di-, and trimeric triazoles based on 2-azabicycloalkanes.
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