TY  - JOUR
AU  - Đukić, Mirjana
AU  - Fesatidou, Mara
AU  - Xenikakis, Iakovos
AU  - Geronikaki, Athina
AU  - Angelova, Violina T.
AU  - Savić, Vladimir
AU  - Pasić, Marta
AU  - Krilović, Branislav
AU  - Đukić, Dušan
AU  - Gobeljić, Borko
AU  - Pavlica, Marina
AU  - Đurić, Ana
AU  - Stanojević, Ivan
AU  - Vojvodić, Danilo
AU  - Saso, Luciano
PY  - 2018
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3154
AB  - The initial steps in preclinical drug developing research concern the synthesis of new compounds for specific therapeutic use which needs to be confirmed by in vitro and then in vivo testing. Nine thiazolidinone derivatives (numerically labeled 1-9) classified as follows: 1,3-thiazole-based compounds (1 and 2); 1,3,4-thiadiazole based compounds (3 and 4); substituted 5-benzylideno-2-adamantylthiazol[3,2-b] [1,2,4] triazol-6(5H) ones (5-8); and an ethylaminothiazole-based chalcone (9), were tested for antioxidant activity (AOA) by using three in vitro assays: DPPH (1,1-diphenyl-2-picrylhydrazyl scavenging capacity test); FRAP (ferric reducing antioxidant power test); and TBARS (thiobarbituric acid reactive substances test). Compounds 1-4 and 9 in particular are newly synthesized compounds. Also, traditional antioxidants Vitamins E and C and alpha-lipoic acid (alpha-LA) were tested. The results of DPPH testing: Vitamin C 94.35%, Vitamin E 2.99% and alpha-LA 1.57%; compounds: 4 33.98%; 2 18.73%; 1 15.62%; 5 6.59%; 3 4.99%; 6-9 demonstrated almost no AOA. The results of TBARS testing (% of LPO inhibition): Vitamin C 62.32%; Vitamin E 36.29%; alpha-LA 51.36%; compounds: 1 62.11%; 5 66.71%; 9 60.93%; 4, 6 and 7 demonstrated similar to 50%; 3 and 8 displayed similar to 38%; 2 23.51%. By FRAP method, Vitamins E and C showed equal AOA, similar to 100%, unlike alpha-LA (no AOA), and AOA of the tested compounds (expressed as a fraction of the AOA of Vitamin C) were: 2 and 4-75%; 8, 3 and 1-45%; 5-7 and 9-27%. Different red-ox reaction principles between these assays dictate different AOA outcomes for a single compound. Vitamin C appeared to be the superior antioxidant out of the traditional antioxidants; and compound 4 was superior to other tested thiazolidinone derivatives. Vitamin C appeared to be the superior antioxidant out of the traditional antioxidants; and compound 4 was superior to other tested thiazolidinone derivatives. Phenyl-functionalized benzylidene, amino-carbonyl functional domains and chelating ligand properties of the thiazolidinone derivatives correlated with AOA.
PB  - Elsevier Ireland Ltd, Clare
T2  - Chemico-Biological Interactions
T1  - In vitro antioxidant activity of thiazolidinone derivatives of 1,3-thiazole and 1,3,4-thiadiazole
VL  - 286
SP  - 119
EP  - 131
DO  - 10.1016/j.cbi.2018.03.013
ER  - 

@article{
author = "Đukić, Mirjana and Fesatidou, Mara and Xenikakis, Iakovos and Geronikaki, Athina and Angelova, Violina T. and Savić, Vladimir and Pasić, Marta and Krilović, Branislav and Đukić, Dušan and Gobeljić, Borko and Pavlica, Marina and Đurić, Ana and Stanojević, Ivan and Vojvodić, Danilo and Saso, Luciano",
year = "2018",
abstract = "The initial steps in preclinical drug developing research concern the synthesis of new compounds for specific therapeutic use which needs to be confirmed by in vitro and then in vivo testing. Nine thiazolidinone derivatives (numerically labeled 1-9) classified as follows: 1,3-thiazole-based compounds (1 and 2); 1,3,4-thiadiazole based compounds (3 and 4); substituted 5-benzylideno-2-adamantylthiazol[3,2-b] [1,2,4] triazol-6(5H) ones (5-8); and an ethylaminothiazole-based chalcone (9), were tested for antioxidant activity (AOA) by using three in vitro assays: DPPH (1,1-diphenyl-2-picrylhydrazyl scavenging capacity test); FRAP (ferric reducing antioxidant power test); and TBARS (thiobarbituric acid reactive substances test). Compounds 1-4 and 9 in particular are newly synthesized compounds. Also, traditional antioxidants Vitamins E and C and alpha-lipoic acid (alpha-LA) were tested. The results of DPPH testing: Vitamin C 94.35%, Vitamin E 2.99% and alpha-LA 1.57%; compounds: 4 33.98%; 2 18.73%; 1 15.62%; 5 6.59%; 3 4.99%; 6-9 demonstrated almost no AOA. The results of TBARS testing (% of LPO inhibition): Vitamin C 62.32%; Vitamin E 36.29%; alpha-LA 51.36%; compounds: 1 62.11%; 5 66.71%; 9 60.93%; 4, 6 and 7 demonstrated similar to 50%; 3 and 8 displayed similar to 38%; 2 23.51%. By FRAP method, Vitamins E and C showed equal AOA, similar to 100%, unlike alpha-LA (no AOA), and AOA of the tested compounds (expressed as a fraction of the AOA of Vitamin C) were: 2 and 4-75%; 8, 3 and 1-45%; 5-7 and 9-27%. Different red-ox reaction principles between these assays dictate different AOA outcomes for a single compound. Vitamin C appeared to be the superior antioxidant out of the traditional antioxidants; and compound 4 was superior to other tested thiazolidinone derivatives. Vitamin C appeared to be the superior antioxidant out of the traditional antioxidants; and compound 4 was superior to other tested thiazolidinone derivatives. Phenyl-functionalized benzylidene, amino-carbonyl functional domains and chelating ligand properties of the thiazolidinone derivatives correlated with AOA.",
publisher = "Elsevier Ireland Ltd, Clare",
journal = "Chemico-Biological Interactions",
title = "In vitro antioxidant activity of thiazolidinone derivatives of 1,3-thiazole and 1,3,4-thiadiazole",
volume = "286",
pages = "119-131",
doi = "10.1016/j.cbi.2018.03.013"
}

Đukić, M., Fesatidou, M., Xenikakis, I., Geronikaki, A., Angelova, V. T., Savić, V., Pasić, M., Krilović, B., Đukić, D., Gobeljić, B., Pavlica, M., Đurić, A., Stanojević, I., Vojvodić, D.,& Saso, L.. (2018). In vitro antioxidant activity of thiazolidinone derivatives of 1,3-thiazole and 1,3,4-thiadiazole. in Chemico-Biological Interactions
Elsevier Ireland Ltd, Clare., 286, 119-131.
https://doi.org/10.1016/j.cbi.2018.03.013

Đukić M, Fesatidou M, Xenikakis I, Geronikaki A, Angelova VT, Savić V, Pasić M, Krilović B, Đukić D, Gobeljić B, Pavlica M, Đurić A, Stanojević I, Vojvodić D, Saso L. In vitro antioxidant activity of thiazolidinone derivatives of 1,3-thiazole and 1,3,4-thiadiazole. in Chemico-Biological Interactions. 2018;286:119-131.
doi:10.1016/j.cbi.2018.03.013 .

Đukić, Mirjana, Fesatidou, Mara, Xenikakis, Iakovos, Geronikaki, Athina, Angelova, Violina T., Savić, Vladimir, Pasić, Marta, Krilović, Branislav, Đukić, Dušan, Gobeljić, Borko, Pavlica, Marina, Đurić, Ana, Stanojević, Ivan, Vojvodić, Danilo, Saso, Luciano, "In vitro antioxidant activity of thiazolidinone derivatives of 1,3-thiazole and 1,3,4-thiadiazole" in Chemico-Biological Interactions, 286 (2018):119-131,
https://doi.org/10.1016/j.cbi.2018.03.013 . .

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 . .

TY  - JOUR
AU  - Aminjafari, Akram
AU  - Miroliaei, Mehran
AU  - Angelova, Violina T.
AU  - Emamzadeh, Rahman
AU  - Đukić, Mirjana
AU  - Đurić, Ana
AU  - Saso, Luciano
PY  - 2016
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/2679
AB  - Background: Synthesized aminocoumarins are heterocyclic compounds possessing potential for the treatment of insulin-dependent diabetes mellitus with unexplored anti-glycative action. Results: In this study 4-aminocoumarin derivatives (4-ACDs) were evaluated in vitro for antiglycation (AG) activities by using the human serum albumin (HSA)/glucose system, for 8 weeks of incubation. The glycation and conformational alteration of HSA in the presence of the tested compounds were evaluated by Congo red assay, fluorescence and circular dichroism spectroscopy. The antioxidant (AO) capacity were also tested by four different assays including: DPPH (2,2'-diphenyl-1-picrylhydrazyl radical), ABTS (2,2-azinobis (3-ethylbenzothiazoline-6-sulphonate) diammonium salt), FRAP (ferric reducing antioxidant power) and beta-carotene-linoleic acid assay. The tested compounds showed AG and AO effects. The intensity of the accomplished AO potential is related to the type of the used assay. Significant alterations in the secondary (monitored by CD spectropolarimetry) and tertiary structure (assessed by spectrofluorimetry) of HSA upon glycation were mitigated by the 4-ACDs, suggesting their suppressive role in the late stage (post-Amadori) of the HSA glycation. Conclusions: By the analogues, in vitro ascertained AO and AG properties of 4-ACDmay be recognized as rationale for their protective role against oxidative changes of proteins, thereby precluding diabetic complications in humans.
PB  - Univ Catolica de Valparaiso, Valparaiso
T2  - Electronic Journal of Biotechnology
T1  - Antioxidant activity and protective role on protein glycation of synthetic aminocoumarins
VL  - 24
SP  - 43
EP  - 48
DO  - 10.1016/j.ejbt.2016.08.004
ER  - 

@article{
author = "Aminjafari, Akram and Miroliaei, Mehran and Angelova, Violina T. and Emamzadeh, Rahman and Đukić, Mirjana and Đurić, Ana and Saso, Luciano",
year = "2016",
abstract = "Background: Synthesized aminocoumarins are heterocyclic compounds possessing potential for the treatment of insulin-dependent diabetes mellitus with unexplored anti-glycative action. Results: In this study 4-aminocoumarin derivatives (4-ACDs) were evaluated in vitro for antiglycation (AG) activities by using the human serum albumin (HSA)/glucose system, for 8 weeks of incubation. The glycation and conformational alteration of HSA in the presence of the tested compounds were evaluated by Congo red assay, fluorescence and circular dichroism spectroscopy. The antioxidant (AO) capacity were also tested by four different assays including: DPPH (2,2'-diphenyl-1-picrylhydrazyl radical), ABTS (2,2-azinobis (3-ethylbenzothiazoline-6-sulphonate) diammonium salt), FRAP (ferric reducing antioxidant power) and beta-carotene-linoleic acid assay. The tested compounds showed AG and AO effects. The intensity of the accomplished AO potential is related to the type of the used assay. Significant alterations in the secondary (monitored by CD spectropolarimetry) and tertiary structure (assessed by spectrofluorimetry) of HSA upon glycation were mitigated by the 4-ACDs, suggesting their suppressive role in the late stage (post-Amadori) of the HSA glycation. Conclusions: By the analogues, in vitro ascertained AO and AG properties of 4-ACDmay be recognized as rationale for their protective role against oxidative changes of proteins, thereby precluding diabetic complications in humans.",
publisher = "Univ Catolica de Valparaiso, Valparaiso",
journal = "Electronic Journal of Biotechnology",
title = "Antioxidant activity and protective role on protein glycation of synthetic aminocoumarins",
volume = "24",
pages = "43-48",
doi = "10.1016/j.ejbt.2016.08.004"
}

Aminjafari, A., Miroliaei, M., Angelova, V. T., Emamzadeh, R., Đukić, M., Đurić, A.,& Saso, L.. (2016). Antioxidant activity and protective role on protein glycation of synthetic aminocoumarins. in Electronic Journal of Biotechnology
Univ Catolica de Valparaiso, Valparaiso., 24, 43-48.
https://doi.org/10.1016/j.ejbt.2016.08.004

Aminjafari A, Miroliaei M, Angelova VT, Emamzadeh R, Đukić M, Đurić A, Saso L. Antioxidant activity and protective role on protein glycation of synthetic aminocoumarins. in Electronic Journal of Biotechnology. 2016;24:43-48.
doi:10.1016/j.ejbt.2016.08.004 .

Aminjafari, Akram, Miroliaei, Mehran, Angelova, Violina T., Emamzadeh, Rahman, Đukić, Mirjana, Đurić, Ana, Saso, Luciano, "Antioxidant activity and protective role on protein glycation of synthetic aminocoumarins" in Electronic Journal of Biotechnology, 24 (2016):43-48,
https://doi.org/10.1016/j.ejbt.2016.08.004 . .

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 . .