Novel Coumarin Derivatives Containing 1,2,4-Triazole, 4,5-Dicyanoimidazole and Purine Moieties: Synthesis and Evaluation of Their Cytostatic Activity
by
Krešimir Benci 1, Leo Mandić 1, Tomislav Suhina 1, Mirela Sedić 2, Marko Klobučar 2, Sandra Kraljević Pavelić 2, Krešimir Pavelić 2, Karlo Wittine 1 and 
Mladen Mintas 1,*
Mladen Mintas 1,*
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.
Molecules 2012, 17(9), 11010-11025; https://doi.org/10.3390/molecules170911010
Received: 16 July 2012 / Revised: 23 August 2012 / Accepted: 3 September 2012 / Published: 12 September 2012
(This article belongs to the Section Medicinal Chemistry)
We report here on the synthesis and in vitro anti-tumor effects of a series of novel 1,2,4-triazole (compounds 3–6), 4,5-dicyanoimidazole (compound 7), and purine (compounds 8–13) coumarin derivatives and their acyclic nucleoside analogues 14–18. Structures of novel compounds 3–18 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.
View Full-Text
Keywords:
1,2,4-triazole; 4,5-dicyanoimidazole and purine coumarin derivatives; acyclic nucleoside analogues; antitumor activity evaluation
▼
Show Figures
Figure 1
This is an open access article distributed under the Creative Commons Attribution License
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.
Show more citation formats
