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Molecules 2012, 17(9), 11010-11025; doi:10.3390/molecules170911010

Novel Coumarin Derivatives Containing 1,2,4-Triazole, 4,5-Dicyanoimidazole and Purine Moieties: Synthesis and Evaluation of Their Cytostatic Activity

1
Department of Organic Chemistry, Faculty of Chemical Engineering and Technology, University of Zagreb, Marulićev trg 19, Zagreb 10000, Croatia
2
Department of Biotechnology, University of Rijeka, Slavka Krautzeka 83 A, Rijeka 51000, Croatia
*
Author to whom correspondence should be addressed.
Received: 16 July 2012 / Revised: 23 August 2012 / Accepted: 3 September 2012 / Published: 12 September 2012
(This article belongs to the Section Medicinal Chemistry)
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Abstract

We report here on the synthesis and in vitro anti-tumor effects of a series of novel 1,2,4-triazole (compounds 36), 4,5-dicyanoimidazole (compound 7), and purine (compounds 813) coumarin derivatives and their acyclic nucleoside analogues 1418. Structures of novel compounds 318 were deduced from their 1H- and 13C-NMR and corresponding mass spectra. Results of anti-proliferative assays performed on a panel of selected human tumor cell lines revealed that compound 6 had moderate cytostatic activity against the HeLa cell line (IC50 = 35 µM), whereas compound 10 showed moderate activity against the HeLa (IC50 = 33 µM), HepG2 (IC50 = 25 µM) and SW620 (IC50 = 35 µM) cell lines. These compounds showed no cytotoxic effects on normal (diploid) human fibroblasts.
Keywords: 1,2,4-triazole; 4,5-dicyanoimidazole and purine coumarin derivatives; acyclic nucleoside analogues; antitumor activity evaluation 1,2,4-triazole; 4,5-dicyanoimidazole and purine coumarin derivatives; acyclic nucleoside analogues; antitumor activity evaluation
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Benci, K.; Mandić, L.; Suhina, T.; Sedić, M.; Klobučar, M.; Kraljević Pavelić, S.; Pavelić, K.; Wittine, K.; Mintas, M. Novel Coumarin Derivatives Containing 1,2,4-Triazole, 4,5-Dicyanoimidazole and Purine Moieties: Synthesis and Evaluation of Their Cytostatic Activity. Molecules 2012, 17, 11010-11025.

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