TY  - JOUR
AU  - Buzharevski, Antonio
AU  - Paskaš, Svetlana
AU  - Sárosi, Menyhárt-Botond
AU  - Laube, Markus
AU  - Lönnecke, Peter
AU  - Neumann, Wilma
AU  - Murganić, Blagoje
AU  - Mijatović, Sanja
AU  - Maksimović-Ivanić, Danijela
AU  - Pietzsch, Jens
AU  - Hey-Hawkins, Evamarie
PY  - 2020
UR  - http://www.ncbi.nlm.nih.gov/pubmed/32179835
UR  - http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=PMC7076013
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/3640
AB  - Owing to the involvement of cyclooxygenase-2 (COX-2) in carcinogenesis, COX-2-selective inhibitors are increasingly studied for their potential cytotoxic properties. Moreover, the incorporation of carboranes in structures of established anti-inflammatory drugs can improve the potency and metabolic stability of the inhibitors. Herein, we report the synthesis of carborane-containing derivatives of rofecoxib that display remarkable cytotoxic or cytostatic activity in the micromolar range with excellent selectivity for melanoma and colon cancer cell lines over normal cells. Furthermore, it was shown that the carborane-modified derivatives of rofecoxib showed different modes of action that were dependent on the cell type.
T2  - Scientific Reports
T1  - Carboranyl Derivatives of Rofecoxib with Cytostatic Activity against Human Melanoma and Colon Cancer Cells.
IS  - 1
VL  - 10
DO  - 10.1038/s41598-020-59059-3
SP  - 4827
ER  - 

@article{
author = "Buzharevski, Antonio and Paskaš, Svetlana and Sárosi, Menyhárt-Botond and Laube, Markus and Lönnecke, Peter and Neumann, Wilma and Murganić, Blagoje and Mijatović, Sanja and Maksimović-Ivanić, Danijela and Pietzsch, Jens and Hey-Hawkins, Evamarie",
year = "2020",
abstract = "Owing to the involvement of cyclooxygenase-2 (COX-2) in carcinogenesis, COX-2-selective inhibitors are increasingly studied for their potential cytotoxic properties. Moreover, the incorporation of carboranes in structures of established anti-inflammatory drugs can improve the potency and metabolic stability of the inhibitors. Herein, we report the synthesis of carborane-containing derivatives of rofecoxib that display remarkable cytotoxic or cytostatic activity in the micromolar range with excellent selectivity for melanoma and colon cancer cell lines over normal cells. Furthermore, it was shown that the carborane-modified derivatives of rofecoxib showed different modes of action that were dependent on the cell type.",
journal = "Scientific Reports",
title = "Carboranyl Derivatives of Rofecoxib with Cytostatic Activity against Human Melanoma and Colon Cancer Cells.",
number = "1",
volume = "10",
doi = "10.1038/s41598-020-59059-3",
pages = "4827"
}

Buzharevski, A., Paskaš, S., Sárosi, M., Laube, M., Lönnecke, P., Neumann, W., Murganić, B., Mijatović, S., Maksimović-Ivanić, D., Pietzsch, J.,& Hey-Hawkins, E.. (2020). Carboranyl Derivatives of Rofecoxib with Cytostatic Activity against Human Melanoma and Colon Cancer Cells.. in Scientific Reports, 10(1), 4827.
https://doi.org/10.1038/s41598-020-59059-3

Buzharevski A, Paskaš S, Sárosi M, Laube M, Lönnecke P, Neumann W, Murganić B, Mijatović S, Maksimović-Ivanić D, Pietzsch J, Hey-Hawkins E. Carboranyl Derivatives of Rofecoxib with Cytostatic Activity against Human Melanoma and Colon Cancer Cells.. in Scientific Reports. 2020;10(1):4827.
doi:10.1038/s41598-020-59059-3 .

Buzharevski, Antonio, Paskaš, Svetlana, Sárosi, Menyhárt-Botond, Laube, Markus, Lönnecke, Peter, Neumann, Wilma, Murganić, Blagoje, Mijatović, Sanja, Maksimović-Ivanić, Danijela, Pietzsch, Jens, Hey-Hawkins, Evamarie, "Carboranyl Derivatives of Rofecoxib with Cytostatic Activity against Human Melanoma and Colon Cancer Cells." in Scientific Reports, 10, no. 1 (2020):4827,
https://doi.org/10.1038/s41598-020-59059-3 . .

TY  - JOUR
AU  - Drača, Dijana
AU  - Mijatović, Sanja
AU  - Krajnović, Tamara
AU  - Kaluđerović, Goran N
AU  - Wessjohann, Ludger A
AU  - Maksimović-Ivanić, Danijela
PY  - 2019
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/3484
UR  - http://ar.iiarjournals.org/content/39/10/5403
AB  - BACKGROUND/AIM Tubugi-1 is a more stable and accessible synthetic counterpart of natural tubulysins. This study aimed to evaluate its cytotoxic potential against anaplastic human melanoma cells. MATERIALS AND METHODS The viability of A-375 cells was determined by 3-(4,5-dimethythiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and crystal violet assay. The type of cell death and proliferative rate were investigated using flow cytometry and fluorescent microscopy, while the molecular background was evaluated by western blot. RESULTS Tubugi-1 reduced the viability of A-375 cells, inducing massive micronucleation, followed by augmented expression of inhibitor of nuclear factor-κB and caspase-2, typical of a mitotic catastrophe. Disturbed proliferation and G2M block with prominent caspase activity, weakened the expression of B-cell lymphoma 2 and B-cell lymphoma 2-associated X transient up-regulation, coexisted with intensive autophagy. Specific inhibition of autophagy by chloroquine resulted in conversion from mitotic catastrophe to rapid apoptosis. CONCLUSION Multilevel anticancer action of tubugi-1 is extended by co-application of an autophagy inhibitor, giving a new dimension in further preclinical advancement of this potential agent.
T2  - Anticancer Research
T1  - Synthetic Tubulysin Derivative, Tubugi-1, Against Invasive Melanoma Cells: The Cell Death Triangle.
IS  - 10
VL  - 39
DO  - 10.21873/anticanres.13734
SP  - 5403
EP  - 5415
ER  - 

@article{
author = "Drača, Dijana and Mijatović, Sanja and Krajnović, Tamara and Kaluđerović, Goran N and Wessjohann, Ludger A and Maksimović-Ivanić, Danijela",
year = "2019",
abstract = "BACKGROUND/AIM Tubugi-1 is a more stable and accessible synthetic counterpart of natural tubulysins. This study aimed to evaluate its cytotoxic potential against anaplastic human melanoma cells. MATERIALS AND METHODS The viability of A-375 cells was determined by 3-(4,5-dimethythiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and crystal violet assay. The type of cell death and proliferative rate were investigated using flow cytometry and fluorescent microscopy, while the molecular background was evaluated by western blot. RESULTS Tubugi-1 reduced the viability of A-375 cells, inducing massive micronucleation, followed by augmented expression of inhibitor of nuclear factor-κB and caspase-2, typical of a mitotic catastrophe. Disturbed proliferation and G2M block with prominent caspase activity, weakened the expression of B-cell lymphoma 2 and B-cell lymphoma 2-associated X transient up-regulation, coexisted with intensive autophagy. Specific inhibition of autophagy by chloroquine resulted in conversion from mitotic catastrophe to rapid apoptosis. CONCLUSION Multilevel anticancer action of tubugi-1 is extended by co-application of an autophagy inhibitor, giving a new dimension in further preclinical advancement of this potential agent.",
journal = "Anticancer Research",
title = "Synthetic Tubulysin Derivative, Tubugi-1, Against Invasive Melanoma Cells: The Cell Death Triangle.",
number = "10",
volume = "39",
doi = "10.21873/anticanres.13734",
pages = "5403-5415"
}

Drača, D., Mijatović, S., Krajnović, T., Kaluđerović, G. N., Wessjohann, L. A.,& Maksimović-Ivanić, D.. (2019). Synthetic Tubulysin Derivative, Tubugi-1, Against Invasive Melanoma Cells: The Cell Death Triangle.. in Anticancer Research, 39(10), 5403-5415.
https://doi.org/10.21873/anticanres.13734

Drača D, Mijatović S, Krajnović T, Kaluđerović GN, Wessjohann LA, Maksimović-Ivanić D. Synthetic Tubulysin Derivative, Tubugi-1, Against Invasive Melanoma Cells: The Cell Death Triangle.. in Anticancer Research. 2019;39(10):5403-5415.
doi:10.21873/anticanres.13734 .

Drača, Dijana, Mijatović, Sanja, Krajnović, Tamara, Kaluđerović, Goran N, Wessjohann, Ludger A, Maksimović-Ivanić, Danijela, "Synthetic Tubulysin Derivative, Tubugi-1, Against Invasive Melanoma Cells: The Cell Death Triangle." in Anticancer Research, 39, no. 10 (2019):5403-5415,
https://doi.org/10.21873/anticanres.13734 . .

TY  - JOUR
AU  - Buzharevski, Antonio
AU  - Paskas, Svetlana
AU  - Sárosi, Menyhárt‐Botond
AU  - Laube, Markus
AU  - Lönnecke, Peter
AU  - Neumann, Wilma
AU  - Mijatović, Sanja
AU  - Maksimović-Ivanić, Danijela
AU  - Pietzsch, Jens
AU  - Hey-Hawkins, Evamarie
PY  - 2019
UR  - https://onlinelibrary.wiley.com/doi/abs/10.1002/cmdc.201800685
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/3254
AB  - Nonsteroidal anti-inflammatory drugs (NSAIDs) are the most common way of treating inflammatory disorders. Their widespread use helped reveal their other modes of action as pharmaceuticals, such as a profound effect on various cancers. Celecoxib has proven to be a very prominent member of this group with cytostatic activities. On the other hand, the highly dynamic field of drug design is constantly searching for new ways of modifying known structures to obtain more powerful and less harmful drugs. A very interesting development is the implementation of carboranes in pharmacologically active structures, mostly as phenyl mimetics. Herein we report the synthesis of three carborane-containing derivatives of the COX-2-selective NSAID celecoxib. The new compounds proved to have promising cytostatic potential against various melanoma and colorectal adenocarcinoma cell lines. Inhibited proliferation accompanied by caspase-independent apoptotic cell death was found to be the main cause of decreased cell viability upon treatment with the most efficient celecoxib analogue, 3 b (4-[5-(1,7-dicarba-closo-dodecaboranyl)-3-trifluoromethyl-1H-pyrazol-1-yl]-1-methylsulfonylbenzene).
T2  - ChemMedChem
T1  - Carboranyl Analogues of Celecoxib with Potent Cytostatic Activity against Human Melanoma and Colon Cancer Cell Lines.
IS  - 3
VL  - 14
DO  - 10.1002/cmdc.201800685
SP  - 315
EP  - 321
ER  - 

@article{
author = "Buzharevski, Antonio and Paskas, Svetlana and Sárosi, Menyhárt‐Botond and Laube, Markus and Lönnecke, Peter and Neumann, Wilma and Mijatović, Sanja and Maksimović-Ivanić, Danijela and Pietzsch, Jens and Hey-Hawkins, Evamarie",
year = "2019",
abstract = "Nonsteroidal anti-inflammatory drugs (NSAIDs) are the most common way of treating inflammatory disorders. Their widespread use helped reveal their other modes of action as pharmaceuticals, such as a profound effect on various cancers. Celecoxib has proven to be a very prominent member of this group with cytostatic activities. On the other hand, the highly dynamic field of drug design is constantly searching for new ways of modifying known structures to obtain more powerful and less harmful drugs. A very interesting development is the implementation of carboranes in pharmacologically active structures, mostly as phenyl mimetics. Herein we report the synthesis of three carborane-containing derivatives of the COX-2-selective NSAID celecoxib. The new compounds proved to have promising cytostatic potential against various melanoma and colorectal adenocarcinoma cell lines. Inhibited proliferation accompanied by caspase-independent apoptotic cell death was found to be the main cause of decreased cell viability upon treatment with the most efficient celecoxib analogue, 3 b (4-[5-(1,7-dicarba-closo-dodecaboranyl)-3-trifluoromethyl-1H-pyrazol-1-yl]-1-methylsulfonylbenzene).",
journal = "ChemMedChem",
title = "Carboranyl Analogues of Celecoxib with Potent Cytostatic Activity against Human Melanoma and Colon Cancer Cell Lines.",
number = "3",
volume = "14",
doi = "10.1002/cmdc.201800685",
pages = "315-321"
}

Buzharevski, A., Paskas, S., Sárosi, M., Laube, M., Lönnecke, P., Neumann, W., Mijatović, S., Maksimović-Ivanić, D., Pietzsch, J.,& Hey-Hawkins, E.. (2019). Carboranyl Analogues of Celecoxib with Potent Cytostatic Activity against Human Melanoma and Colon Cancer Cell Lines.. in ChemMedChem, 14(3), 315-321.
https://doi.org/10.1002/cmdc.201800685

Buzharevski A, Paskas S, Sárosi M, Laube M, Lönnecke P, Neumann W, Mijatović S, Maksimović-Ivanić D, Pietzsch J, Hey-Hawkins E. Carboranyl Analogues of Celecoxib with Potent Cytostatic Activity against Human Melanoma and Colon Cancer Cell Lines.. in ChemMedChem. 2019;14(3):315-321.
doi:10.1002/cmdc.201800685 .

Buzharevski, Antonio, Paskas, Svetlana, Sárosi, Menyhárt‐Botond, Laube, Markus, Lönnecke, Peter, Neumann, Wilma, Mijatović, Sanja, Maksimović-Ivanić, Danijela, Pietzsch, Jens, Hey-Hawkins, Evamarie, "Carboranyl Analogues of Celecoxib with Potent Cytostatic Activity against Human Melanoma and Colon Cancer Cell Lines." in ChemMedChem, 14, no. 3 (2019):315-321,
https://doi.org/10.1002/cmdc.201800685 . .