TY  - JOUR
AU  - Simić, Milena
AU  - Petković, Milos
AU  - Jovanović, Predrag
AU  - Jovanović, Milos
AU  - Tasić, Gordana
AU  - Besu, Irina
AU  - Zizak, Zeljko
AU  - Aleksić, Ivana
AU  - Nikodinović-Runić, Jasmina
AU  - Savić, Vladimir
PY  - 2021
UR  - https://imagine.imgge.bg.ac.rs/handle/123456789/1499
AB  - Several coumarin derivatives with a directly attached azole substituent at C-4 were synthesized and biologically studied for their anticancer properties. The cell lines used for this investigation (HeLa, K-562, MDA-MB-53, and MCF-7) demonstrated different sensitivities. The best response in the MTT (3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide) assay was shown by K-562 cells, with compounds displaying activity (3c, IC50 3.06 mu M; 4a, IC50 5.24 mu M; 4c, IC50 4.7 mu M) similar to that of cisplatin (IC50 similar to 6 mu M), which was used as the standard. The studied azole-substituted coumarins demonstrated weaker activity toward other cell lines, except for compound 4c, which was equally potent in the case of MCF-7 cells. Additional biological evaluations supported interference with the cell cycle as a potential mechanism of action and confirmed the absence of toxicity in zebrafish embryos. On the basis of these initial results, 4-azole coumarins should be explored further. Although their activity would need additional optimization, the fact that these compounds are fragment-like structures with MW P  lt 3 offers enough flexibility to fine-tune their drug-like properties.
PB  - Wiley-V C H Verlag Gmbh, Weinheim
T2  - Archiv Der Pharmazie
T1  - Fragment-type 4-azolylcoumarin derivatives with anticancer properties
IS  - 11
VL  - 354
DO  - 10.1002/ardp.202100238
ER  - 

@article{
author = "Simić, Milena and Petković, Milos and Jovanović, Predrag and Jovanović, Milos and Tasić, Gordana and Besu, Irina and Zizak, Zeljko and Aleksić, Ivana and Nikodinović-Runić, Jasmina and Savić, Vladimir",
year = "2021",
abstract = "Several coumarin derivatives with a directly attached azole substituent at C-4 were synthesized and biologically studied for their anticancer properties. The cell lines used for this investigation (HeLa, K-562, MDA-MB-53, and MCF-7) demonstrated different sensitivities. The best response in the MTT (3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide) assay was shown by K-562 cells, with compounds displaying activity (3c, IC50 3.06 mu M; 4a, IC50 5.24 mu M; 4c, IC50 4.7 mu M) similar to that of cisplatin (IC50 similar to 6 mu M), which was used as the standard. The studied azole-substituted coumarins demonstrated weaker activity toward other cell lines, except for compound 4c, which was equally potent in the case of MCF-7 cells. Additional biological evaluations supported interference with the cell cycle as a potential mechanism of action and confirmed the absence of toxicity in zebrafish embryos. On the basis of these initial results, 4-azole coumarins should be explored further. Although their activity would need additional optimization, the fact that these compounds are fragment-like structures with MW P  lt 3 offers enough flexibility to fine-tune their drug-like properties.",
publisher = "Wiley-V C H Verlag Gmbh, Weinheim",
journal = "Archiv Der Pharmazie",
title = "Fragment-type 4-azolylcoumarin derivatives with anticancer properties",
number = "11",
volume = "354",
doi = "10.1002/ardp.202100238"
}

Simić, M., Petković, M., Jovanović, P., Jovanović, M., Tasić, G., Besu, I., Zizak, Z., Aleksić, I., Nikodinović-Runić, J.,& Savić, V.. (2021). Fragment-type 4-azolylcoumarin derivatives with anticancer properties. in Archiv Der Pharmazie
Wiley-V C H Verlag Gmbh, Weinheim., 354(11).
https://doi.org/10.1002/ardp.202100238

Simić M, Petković M, Jovanović P, Jovanović M, Tasić G, Besu I, Zizak Z, Aleksić I, Nikodinović-Runić J, Savić V. Fragment-type 4-azolylcoumarin derivatives with anticancer properties. in Archiv Der Pharmazie. 2021;354(11).
doi:10.1002/ardp.202100238 .

Simić, Milena, Petković, Milos, Jovanović, Predrag, Jovanović, Milos, Tasić, Gordana, Besu, Irina, Zizak, Zeljko, Aleksić, Ivana, Nikodinović-Runić, Jasmina, Savić, Vladimir, "Fragment-type 4-azolylcoumarin derivatives with anticancer properties" in Archiv Der Pharmazie, 354, no. 11 (2021),
https://doi.org/10.1002/ardp.202100238 . .