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基于2-氮杂双环烷烃的三唑类化合物的合成及其抗增殖活性

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

作者信息

Steppeler Franz, Kłopotowska Dagmara, Wietrzyk Joanna, Wojaczyńska Elżbieta

机构信息

Faculty of Chemistry, Wrocław University of Science and Technology, Wybrzeże Wyspiańskiego 27, 50-370 Wrocław, Poland.

Hirszfeld Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, ul. Rudolfa Weigla 12, 53-114 Wrocław, Poland.

出版信息

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

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.

摘要

设计并合成了一个包含21种新型手性1,2,3-三唑基2-氮杂双环烷烃共轭物的文库,该反应采用铜(I)催化的点击反应。评估了所得杂化物对三种选定的人类癌细胞系的抗增殖能力:Hs294T(黑色素瘤)、MIA PaCa-2(胰腺肿瘤)和NCI-H1581(肺肿瘤)。大多数合成化合物表现出中度至强效活性,其中一些化合物比顺铂更具选择性,选择性指数超过9。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f0e8/8072719/d84823cacc55/materials-14-02039-g001.jpg

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