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Synthesis and Antiproliferative Activity of Triazoles Based on 2-Azabicycloalkanes.

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.

SUBMITTER: Steppeler F

PROVIDER: S-EPMC8072719 | biostudies-literature | 2021 Apr

REPOSITORIES: biostudies-literature

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Synthesis and Antiproliferative Activity of Triazoles Based on 2-Azabicycloalkanes.

Steppeler Franz F Kłopotowska Dagmara D Wietrzyk Joanna J Wojaczyńska Elżbieta E

Materials (Basel, Switzerland) 20210418 8

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 selec ...[more]

PMID: 33919613

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