Synthesis and biological profiling of novel isocoumarin derivatives and related compounds Scientific paper

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Milena Radovan Simić
Slavica Erić
Ivan Borić
Annamaria Lubelska
Gniewomir Latacz
Katarzyna Kieć-Kononowicz
Sandra Vojnović
Jasmina Nikodinović-Runić
Vladimir Savić


In the continuation of our study of substituted isocoumarins a series of novel 3-azolyl isocoumarin and their thio derivatives, including some related lactone compounds was prepared and biologically profiled against C. albicans showing moderate activity with MIC values in range of 4–60 mg mL-1, in gen­eral. The additional characterisation of selected compounds was carried out by exploring their activity on CYP3A4 and CYP2D6 enzymes, while experi­ments on mutagenicity were performed by AMES test. The representative isocoum­arins 3b, 4a and 4b showed lower inhibitory activity on CYP enzymes, when compared to the reference inhibitors, ketoconazole and quinidine. Com­pound 4a showed a higher mutagenic potential than the other two compounds. Further characterization included cytotoxicity profiling against normal MRC5 cells.

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How to Cite
M. R. Simić, “Synthesis and biological profiling of novel isocoumarin derivatives and related compounds: Scientific paper”, J. Serb. Chem. Soc., vol. 86, no. 7-8, pp. 639-649, Aug. 2021.
Organic Chemistry


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