Synthesis and biological profiling of novel isocoumarin derivatives and related compounds
Authors
Simić, Milena R.Erić, Slavica
Borić, Ivan
Lubelska, Annamaria
Latacz, Gniewomir
Kiec-Kononowicz, Katarzyna
Vojnović, Sandra
Nikodinović-Runić, Jasmina
Savić, Vladimir M.
Article (Published version)
Metadata
Show full item recordAbstract
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 mu g 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.
Keywords:
isocoumarins / CYP enzymes / Candida albicans / antifungal compounds / AMESSource:
Journal of the Serbian Chemical Society, 2021, 86, 7-8, 639-649Publisher:
- Srpsko hemijsko društvo, Beograd
Funding / projects:
- Ministry of Science, Technological Development and Innovation of the Republic of Serbia, institutional funding - 200161 (University of Belgrade, Faculty of Pharmacy) (RS-MESTD-inst-2020-200161)
- Ministry of Science, Technological Development and Innovation of the Republic of Serbia, institutional funding - 200042 (University of Belgrade, Institute of Molecular Genetics and Genetic Engineering) (RS-MESTD-inst-2020-200042)
DOI: 10.2298/JSC201201025S
ISSN: 0352-5139
WoS: 000683749400002
Scopus: 2-s2.0-85112083788
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Institut za molekularnu genetiku i genetičko inženjerstvoTY - JOUR AU - Simić, Milena R. AU - Erić, Slavica AU - Borić, Ivan AU - Lubelska, Annamaria AU - Latacz, Gniewomir AU - Kiec-Kononowicz, Katarzyna AU - Vojnović, Sandra AU - Nikodinović-Runić, Jasmina AU - Savić, Vladimir M. PY - 2021 UR - https://imagine.imgge.bg.ac.rs/handle/123456789/1498 AB - 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 mu g 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. PB - Srpsko hemijsko društvo, Beograd T2 - Journal of the Serbian Chemical Society T1 - Synthesis and biological profiling of novel isocoumarin derivatives and related compounds EP - 649 IS - 7-8 SP - 639 VL - 86 DO - 10.2298/JSC201201025S ER -
@article{ author = "Simić, Milena R. and Erić, Slavica and Borić, Ivan and Lubelska, Annamaria and Latacz, Gniewomir and Kiec-Kononowicz, Katarzyna and Vojnović, Sandra and Nikodinović-Runić, Jasmina and Savić, Vladimir M.", year = "2021", abstract = "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 mu g 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.", publisher = "Srpsko hemijsko društvo, Beograd", journal = "Journal of the Serbian Chemical Society", title = "Synthesis and biological profiling of novel isocoumarin derivatives and related compounds", pages = "649-639", number = "7-8", volume = "86", doi = "10.2298/JSC201201025S" }
Simić, M. R., Erić, S., Borić, I., Lubelska, A., Latacz, G., Kiec-Kononowicz, K., Vojnović, S., Nikodinović-Runić, J.,& Savić, V. M.. (2021). Synthesis and biological profiling of novel isocoumarin derivatives and related compounds. in Journal of the Serbian Chemical Society Srpsko hemijsko društvo, Beograd., 86(7-8), 639-649. https://doi.org/10.2298/JSC201201025S
Simić MR, Erić S, Borić I, Lubelska A, Latacz G, Kiec-Kononowicz K, Vojnović S, Nikodinović-Runić J, Savić VM. Synthesis and biological profiling of novel isocoumarin derivatives and related compounds. in Journal of the Serbian Chemical Society. 2021;86(7-8):639-649. doi:10.2298/JSC201201025S .
Simić, Milena R., Erić, Slavica, Borić, Ivan, Lubelska, Annamaria, Latacz, Gniewomir, Kiec-Kononowicz, Katarzyna, Vojnović, Sandra, Nikodinović-Runić, Jasmina, Savić, Vladimir M., "Synthesis and biological profiling of novel isocoumarin derivatives and related compounds" in Journal of the Serbian Chemical Society, 86, no. 7-8 (2021):639-649, https://doi.org/10.2298/JSC201201025S . .