Fragment-type 4-azolylcoumarin derivatives with anticancer properties
| Autor: | Irina Besu, Gordana Tasic, Milos Petkovic, Jasmina Nikodinovic-Runic, Predrag Jovanović, Milos Jovanovic, Vladimir Savic, Zeljko Zizak, Ivana Aleksic, Milena Simic |
|---|---|
| Rok vydání: | 2021 |
| Předmět: |
Male
embryotoxicity azoles Substituent Pharmaceutical Science Antineoplastic Agents cell lines 01 natural sciences HeLa 03 medical and health sciences chemistry.chemical_compound Inhibitory Concentration 50 Structure-Activity Relationship Bromide Coumarins Cell Line Tumor Neoplasms Drug Discovery Toxicity Tests Animals Humans IC50 Zebrafish 030304 developmental biology chemistry.chemical_classification 0303 health sciences coumarins biology 010405 organic chemistry Cell Cycle anticancer properties Cell cycle biology.organism_classification Coumarin Combinatorial chemistry 3. Good health 0104 chemical sciences chemistry Cell culture MCF-7 Cells Azole Female Cisplatin K562 Cells HeLa Cells |
| Zdroj: | Archiv der Pharmazie |
| ISSN: | 1521-4184 |
| Popis: | 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 μM; 4a, IC50 5.24 μM; 4c, IC50 4.7 μM) similar to that of cisplatin (IC50 ~6 μM), 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 |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Plný text