TY  - JOUR
AU  - Svircev, Milos
AU  - Popsavin, Mirjana
AU  - Pavić, Aleksandar
AU  - Vasiljević, Branka
AU  - Rodić, Marko V.
AU  - Đokić, Sanja
AU  - Kesić, Jelena
AU  - Sreco Zelenović, Bojana
AU  - Popsavin, Velimir
AU  - Kojić, Vesna
PY  - 2022
UR  - https://imagine.imgge.bg.ac.rs/handle/123456789/1582
PB  - Academic Press Inc Elsevier Science, San Diego
T2  - Bioorganic Chemistry
T1  - Design, synthesis, and biological evaluation of thiazole bioisosteres of goniofufurone through in vitro antiproliferative activity and in vivo toxicity (vol 121, 105691, 2022)
VL  - 127
DO  - 10.1016/j.bioorg.2022.105984
ER  - 

@article{
author = "Svircev, Milos and Popsavin, Mirjana and Pavić, Aleksandar and Vasiljević, Branka and Rodić, Marko V. and Đokić, Sanja and Kesić, Jelena and Sreco Zelenović, Bojana and Popsavin, Velimir and Kojić, Vesna",
year = "2022",
publisher = "Academic Press Inc Elsevier Science, San Diego",
journal = "Bioorganic Chemistry",
title = "Design, synthesis, and biological evaluation of thiazole bioisosteres of goniofufurone through in vitro antiproliferative activity and in vivo toxicity (vol 121, 105691, 2022)",
volume = "127",
doi = "10.1016/j.bioorg.2022.105984"
}

Svircev, M., Popsavin, M., Pavić, A., Vasiljević, B., Rodić, M. V., Đokić, S., Kesić, J., Sreco Zelenović, B., Popsavin, V.,& Kojić, V.. (2022). Design, synthesis, and biological evaluation of thiazole bioisosteres of goniofufurone through in vitro antiproliferative activity and in vivo toxicity (vol 121, 105691, 2022). in Bioorganic Chemistry
Academic Press Inc Elsevier Science, San Diego., 127.
https://doi.org/10.1016/j.bioorg.2022.105984

Svircev M, Popsavin M, Pavić A, Vasiljević B, Rodić MV, Đokić S, Kesić J, Sreco Zelenović B, Popsavin V, Kojić V. Design, synthesis, and biological evaluation of thiazole bioisosteres of goniofufurone through in vitro antiproliferative activity and in vivo toxicity (vol 121, 105691, 2022). in Bioorganic Chemistry. 2022;127.
doi:10.1016/j.bioorg.2022.105984 .

Svircev, Milos, Popsavin, Mirjana, Pavić, Aleksandar, Vasiljević, Branka, Rodić, Marko V., Đokić, Sanja, Kesić, Jelena, Sreco Zelenović, Bojana, Popsavin, Velimir, Kojić, Vesna, "Design, synthesis, and biological evaluation of thiazole bioisosteres of goniofufurone through in vitro antiproliferative activity and in vivo toxicity (vol 121, 105691, 2022)" in Bioorganic Chemistry, 127 (2022),
https://doi.org/10.1016/j.bioorg.2022.105984 . .

TY  - JOUR
AU  - Svircev, Milos
AU  - Popsavin, Mirjana
AU  - Pavić, Aleksandar
AU  - Vasiljević, Branka
AU  - Rodić, Marko V.
AU  - Đokić, Sanja
AU  - Kesić, Jelena
AU  - Sreco Zelenović, Bojana
AU  - Popsavin, Velimir
AU  - Kojić, Vesna
PY  - 2022
UR  - https://imagine.imgge.bg.ac.rs/handle/123456789/1561
AB  - The synthesis of several new goniofufurone bioisosteres was achieved in which the phenyl residue was replaced by a thiazole ring. The key steps of the synthesis included the initial condensation of cyanohydrin benzoates with cysteine ethyl ester hydrochloride, followed by the subsequent reaction of resulting C-4 ' epimeric thiazolines with DBU, to introduce 5-deoxy functionality and to elaborate the thiazole ring in one step. Synthesized compounds showed potent growth inhibitory effects against selected human tumour cell lines, especially bioisostere 4, which in the culture of MCF-7 cells displayed the highest activity (IC50 = 0.19 nM) of all compounds under evaluation. This molecule exhibited 64474-fold higher antiproliferative activity than lead 2 and was1053-fold more active than the commercial antitumour agent doxorubicin in the culture of MCF-7 cells. The structural features of the tested compounds responsible for their antiproliferative activity have been identified by preliminary SAR analysis. The toxicity of the most active compound 4 was assessed by an in vivo experiment in a zebrafish model (Danio rerio), whereupon it was found non-toxic at any of the tested concentrations up to 125 mu M.
PB  - Academic Press Inc Elsevier Science, San Diego
T2  - Bioorganic Chemistry
T1  - Design, synthesis, and biological evaluation of thiazole bioisosteres of goniofufurone through in vitro antiproliferative activity and in vivo toxicity
VL  - 121
DO  - 10.1016/j.bioorg.2022.105691
ER  - 

@article{
author = "Svircev, Milos and Popsavin, Mirjana and Pavić, Aleksandar and Vasiljević, Branka and Rodić, Marko V. and Đokić, Sanja and Kesić, Jelena and Sreco Zelenović, Bojana and Popsavin, Velimir and Kojić, Vesna",
year = "2022",
abstract = "The synthesis of several new goniofufurone bioisosteres was achieved in which the phenyl residue was replaced by a thiazole ring. The key steps of the synthesis included the initial condensation of cyanohydrin benzoates with cysteine ethyl ester hydrochloride, followed by the subsequent reaction of resulting C-4 ' epimeric thiazolines with DBU, to introduce 5-deoxy functionality and to elaborate the thiazole ring in one step. Synthesized compounds showed potent growth inhibitory effects against selected human tumour cell lines, especially bioisostere 4, which in the culture of MCF-7 cells displayed the highest activity (IC50 = 0.19 nM) of all compounds under evaluation. This molecule exhibited 64474-fold higher antiproliferative activity than lead 2 and was1053-fold more active than the commercial antitumour agent doxorubicin in the culture of MCF-7 cells. The structural features of the tested compounds responsible for their antiproliferative activity have been identified by preliminary SAR analysis. The toxicity of the most active compound 4 was assessed by an in vivo experiment in a zebrafish model (Danio rerio), whereupon it was found non-toxic at any of the tested concentrations up to 125 mu M.",
publisher = "Academic Press Inc Elsevier Science, San Diego",
journal = "Bioorganic Chemistry",
title = "Design, synthesis, and biological evaluation of thiazole bioisosteres of goniofufurone through in vitro antiproliferative activity and in vivo toxicity",
volume = "121",
doi = "10.1016/j.bioorg.2022.105691"
}

Svircev, M., Popsavin, M., Pavić, A., Vasiljević, B., Rodić, M. V., Đokić, S., Kesić, J., Sreco Zelenović, B., Popsavin, V.,& Kojić, V.. (2022). Design, synthesis, and biological evaluation of thiazole bioisosteres of goniofufurone through in vitro antiproliferative activity and in vivo toxicity. in Bioorganic Chemistry
Academic Press Inc Elsevier Science, San Diego., 121.
https://doi.org/10.1016/j.bioorg.2022.105691

Svircev M, Popsavin M, Pavić A, Vasiljević B, Rodić MV, Đokić S, Kesić J, Sreco Zelenović B, Popsavin V, Kojić V. Design, synthesis, and biological evaluation of thiazole bioisosteres of goniofufurone through in vitro antiproliferative activity and in vivo toxicity. in Bioorganic Chemistry. 2022;121.
doi:10.1016/j.bioorg.2022.105691 .

Svircev, Milos, Popsavin, Mirjana, Pavić, Aleksandar, Vasiljević, Branka, Rodić, Marko V., Đokić, Sanja, Kesić, Jelena, Sreco Zelenović, Bojana, Popsavin, Velimir, Kojić, Vesna, "Design, synthesis, and biological evaluation of thiazole bioisosteres of goniofufurone through in vitro antiproliferative activity and in vivo toxicity" in Bioorganic Chemistry, 121 (2022),
https://doi.org/10.1016/j.bioorg.2022.105691 . .