National Research Fund of Bulgaria - UNA-17/2005

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National Research Fund of Bulgaria - UNA-17/2005

Authors

Publications

Antimycobacterial activity of novel hydrazide-hydrazone derivatives with 2H-chromene and coumarin scaffold

Angelova, Violina T.; Valcheva, Violeta; Vassilev, Nikolay G.; Buyukliev, Rosen; Momekov, Georgi; Dimitrov, Ivan; Saso, Luciano; Đukić, Mirjana; Shivachev, Boris

(Pergamon-Elsevier Science Ltd, Oxford, 2017)

TY  - JOUR
AU  - Angelova, Violina T.
AU  - Valcheva, Violeta
AU  - Vassilev, Nikolay G.
AU  - Buyukliev, Rosen
AU  - Momekov, Georgi
AU  - Dimitrov, Ivan
AU  - Saso, Luciano
AU  - Đukić, Mirjana
AU  - Shivachev, Boris
PY  - 2017
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2940
AB  - This study reports the synthesis of new 2H-chromene or coumarin based acylhydrazones, which were evaluated for their in vitro antimycobacterial activity against reference strain Mycobacterium tuberculosis H37Rv and compared to the first-line antituberculosis drugs, isoniazid (INH) and ethambutol (EMB). The most active compounds 7m (MIC 0.13 mu M), 7o (MIC 0.15 mu M) and 7k (MIC 0.17 mu M) demonstrated antimycobacterial activity at submicromolar concentration level and remarkably minimal associated cytotoxicity in the human embryonic kidney cell line HEK-293T. Structure-activity relationship for this class of compounds has been established.
PB  - Pergamon-Elsevier Science Ltd, Oxford
T2  - Bioorganic & Medicinal Chemistry Letters
T1  - Antimycobacterial activity of novel hydrazide-hydrazone derivatives with 2H-chromene and coumarin scaffold
VL  - 27
IS  - 2
SP  - 223
EP  - 227
DO  - 10.1016/j.bmcl.2016.11.071
ER  - 
@article{
author = "Angelova, Violina T. and Valcheva, Violeta and Vassilev, Nikolay G. and Buyukliev, Rosen and Momekov, Georgi and Dimitrov, Ivan and Saso, Luciano and Đukić, Mirjana and Shivachev, Boris",
year = "2017",
abstract = "This study reports the synthesis of new 2H-chromene or coumarin based acylhydrazones, which were evaluated for their in vitro antimycobacterial activity against reference strain Mycobacterium tuberculosis H37Rv and compared to the first-line antituberculosis drugs, isoniazid (INH) and ethambutol (EMB). The most active compounds 7m (MIC 0.13 mu M), 7o (MIC 0.15 mu M) and 7k (MIC 0.17 mu M) demonstrated antimycobacterial activity at submicromolar concentration level and remarkably minimal associated cytotoxicity in the human embryonic kidney cell line HEK-293T. Structure-activity relationship for this class of compounds has been established.",
publisher = "Pergamon-Elsevier Science Ltd, Oxford",
journal = "Bioorganic & Medicinal Chemistry Letters",
title = "Antimycobacterial activity of novel hydrazide-hydrazone derivatives with 2H-chromene and coumarin scaffold",
volume = "27",
number = "2",
pages = "223-227",
doi = "10.1016/j.bmcl.2016.11.071"
}
Angelova, V. T., Valcheva, V., Vassilev, N. G., Buyukliev, R., Momekov, G., Dimitrov, I., Saso, L., Đukić, M.,& Shivachev, B.. (2017). Antimycobacterial activity of novel hydrazide-hydrazone derivatives with 2H-chromene and coumarin scaffold. in Bioorganic & Medicinal Chemistry Letters
Pergamon-Elsevier Science Ltd, Oxford., 27(2), 223-227.
https://doi.org/10.1016/j.bmcl.2016.11.071
Angelova VT, Valcheva V, Vassilev NG, Buyukliev R, Momekov G, Dimitrov I, Saso L, Đukić M, Shivachev B. Antimycobacterial activity of novel hydrazide-hydrazone derivatives with 2H-chromene and coumarin scaffold. in Bioorganic & Medicinal Chemistry Letters. 2017;27(2):223-227.
doi:10.1016/j.bmcl.2016.11.071 .
Angelova, Violina T., Valcheva, Violeta, Vassilev, Nikolay G., Buyukliev, Rosen, Momekov, Georgi, Dimitrov, Ivan, Saso, Luciano, Đukić, Mirjana, Shivachev, Boris, "Antimycobacterial activity of novel hydrazide-hydrazone derivatives with 2H-chromene and coumarin scaffold" in Bioorganic & Medicinal Chemistry Letters, 27, no. 2 (2017):223-227,
https://doi.org/10.1016/j.bmcl.2016.11.071 . .
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Antiproliferative and antioxidative effects of novel hydrazone derivatives bearing coumarin and chromene moiety

Angelova, Violina T.; Vassilev, Nikolay G.; Nikolova-Mladenova, Boryana; Vitas, Jasmina; Malbasa, Radomir; Momekov, Georgi; Đukić, Mirjana; Saso, Luciano

(Springer Birkhauser, New York, 2016)

TY  - JOUR
AU  - Angelova, Violina T.
AU  - Vassilev, Nikolay G.
AU  - Nikolova-Mladenova, Boryana
AU  - Vitas, Jasmina
AU  - Malbasa, Radomir
AU  - Momekov, Georgi
AU  - Đukić, Mirjana
AU  - Saso, Luciano
PY  - 2016
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2760
AB  - A series of new hybrid molecules with a hydrazone fragment were synthesized and characterized by Fourier transform-infrared spectroscopy, nuclear magnetic resonance, mass spectrometry, and elemental analysis. The nuclear magnetic resonance spectra of the hydrazones 4a-c showed exchange of syn and antiperiplanar conformers around the amide bond, the more stable being the antiperiplanar one. The nuclear Overhauser effect spectroscopy (NOESY) spectra confirm E configuration around C=N bond. The tested compounds exhibited concentration-dependent cytotoxic effects against human tumor cell lines in a micromolar range (MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) tetrazolium reduction assay). Hydrazone 4a proved to be the most potent antiproliferative agent of the series. Within the antioxidant screening 8b exhibited the highest radical scavenging activity (% RSA max) and the largest rate constant for the reaction with 2,2-diphenyl-1-picrylhydrazyl.
PB  - Springer Birkhauser, New York
T2  - Medicinal Chemistry Research
T1  - Antiproliferative and antioxidative effects of novel hydrazone derivatives bearing coumarin and chromene moiety
VL  - 25
IS  - 9
SP  - 2082
EP  - 2092
DO  - 10.1007/s00044-016-1661-4
ER  - 
@article{
author = "Angelova, Violina T. and Vassilev, Nikolay G. and Nikolova-Mladenova, Boryana and Vitas, Jasmina and Malbasa, Radomir and Momekov, Georgi and Đukić, Mirjana and Saso, Luciano",
year = "2016",
abstract = "A series of new hybrid molecules with a hydrazone fragment were synthesized and characterized by Fourier transform-infrared spectroscopy, nuclear magnetic resonance, mass spectrometry, and elemental analysis. The nuclear magnetic resonance spectra of the hydrazones 4a-c showed exchange of syn and antiperiplanar conformers around the amide bond, the more stable being the antiperiplanar one. The nuclear Overhauser effect spectroscopy (NOESY) spectra confirm E configuration around C=N bond. The tested compounds exhibited concentration-dependent cytotoxic effects against human tumor cell lines in a micromolar range (MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) tetrazolium reduction assay). Hydrazone 4a proved to be the most potent antiproliferative agent of the series. Within the antioxidant screening 8b exhibited the highest radical scavenging activity (% RSA max) and the largest rate constant for the reaction with 2,2-diphenyl-1-picrylhydrazyl.",
publisher = "Springer Birkhauser, New York",
journal = "Medicinal Chemistry Research",
title = "Antiproliferative and antioxidative effects of novel hydrazone derivatives bearing coumarin and chromene moiety",
volume = "25",
number = "9",
pages = "2082-2092",
doi = "10.1007/s00044-016-1661-4"
}
Angelova, V. T., Vassilev, N. G., Nikolova-Mladenova, B., Vitas, J., Malbasa, R., Momekov, G., Đukić, M.,& Saso, L.. (2016). Antiproliferative and antioxidative effects of novel hydrazone derivatives bearing coumarin and chromene moiety. in Medicinal Chemistry Research
Springer Birkhauser, New York., 25(9), 2082-2092.
https://doi.org/10.1007/s00044-016-1661-4
Angelova VT, Vassilev NG, Nikolova-Mladenova B, Vitas J, Malbasa R, Momekov G, Đukić M, Saso L. Antiproliferative and antioxidative effects of novel hydrazone derivatives bearing coumarin and chromene moiety. in Medicinal Chemistry Research. 2016;25(9):2082-2092.
doi:10.1007/s00044-016-1661-4 .
Angelova, Violina T., Vassilev, Nikolay G., Nikolova-Mladenova, Boryana, Vitas, Jasmina, Malbasa, Radomir, Momekov, Georgi, Đukić, Mirjana, Saso, Luciano, "Antiproliferative and antioxidative effects of novel hydrazone derivatives bearing coumarin and chromene moiety" in Medicinal Chemistry Research, 25, no. 9 (2016):2082-2092,
https://doi.org/10.1007/s00044-016-1661-4 . .
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