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Design, Synthesis, Spectroscopic Characterisation and In Vitro Cytostatic Evaluation of Novel Bis(coumarin-1,2,3-triazolyl)benzenes and Hybrid Coumarin-1,2,3-triazolyl-aryl Derivatives.


ABSTRACT: In this work, a series of novel 1,2,3-triazolyl-coumarin hybrid systems were designed as potential antitumour agents. The structural modification of the coumarin ring was carried out by Cu(I)-catalysed Huisgen 1,3-dipolar cycloaddition of 7-azido-4-methylcoumarin and terminal aromatic alkynes to obtain 1,4-disubstituted 1,2,3-triazolyl-coumarin conjugates 2a-g, bis(1,2,3-triazolyl-coumarin)benzenes 2h-i and coumarin-1,2,3-triazolyl-benzazole hybrids 4a-b. The newly synthesised hybrid molecules were investigated for in vitro antitumour activity against five human cancer cell lines, colon carcinoma HCT116, breast carcinoma MCF-7, lung carcinoma H 460, human T-lymphocyte cells CEM, cervix carcinoma cells HeLa, as well as human dermal microvascular endothelial cells (HMEC-1). Most of these compounds showed moderate to pronounced cytotoxic activity, especially towards MCF-7 cell lines with IC50 = 0.3-32 μM. In addition, compounds 2a-i and 4a-b were studied by UV-Vis absorption and fluorescence spectroscopy and their basic photophysical parameters were determined.

SUBMITTER: Prsir K 

PROVIDER: S-EPMC8840664 | biostudies-literature | 2022 Jan

REPOSITORIES: biostudies-literature

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Design, Synthesis, Spectroscopic Characterisation and In Vitro Cytostatic Evaluation of Novel Bis(coumarin-1,2,3-triazolyl)benzenes and Hybrid Coumarin-1,2,3-triazolyl-aryl Derivatives.

Pršir Kristina K   Horak Ema E   Kralj Marijeta M   Uzelac Lidija L   Liekens Sandra S   Steinberg Ivana Murković IM   Krištafor Svjetlana S  

Molecules (Basel, Switzerland) 20220119 3


In this work, a series of novel 1,2,3-triazolyl-coumarin hybrid systems were designed as potential antitumour agents. The structural modification of the coumarin ring was carried out by Cu(I)-catalysed Huisgen 1,3-dipolar cycloaddition of 7-azido-4-methylcoumarin and terminal aromatic alkynes to obtain 1,4-disubstituted 1,2,3-triazolyl-coumarin conjugates <b>2a</b>-<b>g</b>, bis(1,2,3-triazolyl-coumarin)benzenes <b>2h</b>-<b>i</b> and coumarin-1,2,3-triazolyl-benzazole hybrids <b>4a</b>-<b>b</b>  ...[more]

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2023-03-11 | PXD033004 | Pride