TY  - JOUR
AU  - Vitorović-Todorović, Maja D.
AU  - Erić-Nikolić, Aleksandra
AU  - Kolundžija, Branka
AU  - Hamel, Ernest
AU  - Ristić, Slavica S.
AU  - Juranić, Ivan
AU  - Drakulić, Branko
PY  - 2013
UR  - https://cer.ihtm.bg.ac.rs/handle/123456789/2873
AB  - Antiproliferative activity of twenty-nine (E)-4-aryl-4-oxo-2-butenoic acid amides against three human
tumor cell lines (HeLa, FemX, and K562) is reported. Compounds showed antiproliferative activity in
one-digit micromolar to submicromolar concentrations. The most active derivatives toward all the cell
lines tested bear alkyl substituents on the aroyl moiety of the molecules. Fourteen compounds showed
tubulin assembly inhibition at concentrations <20 mM. The most potent inhibitor of tubulin assembly
was unsubstituted compound 1, with IC50 ¼ 2.9 mM. Compound 23 had an oral LD50 in vivo of 45 mg/kg in
mice. Cell cycle analysis on K562 cells showed that compounds 1, 2 and 23 caused accumulation of cells
in the G2/M phase, but inhibition of microtubule polymerization is not the principal mode of action of
the compounds. Nevertheless, they may be useful leads for the design of a new class of antitubulin
agents.
PB  - Elsevier Masson SAS.
T2  - European Journal of Medicinal Chemistry
T1  - (E)-4-Aryl-4-oxo-2-butenoic acid amides, chalconeearoylacrylic acid chimeras: Design, antiproliferative activity and inhibition of tubulin polymerization
VL  - 62
SP  - 40
EP  - 50
DO  - 10.1016/j.ejmech.2013.01.006
ER  - 

@article{
author = "Vitorović-Todorović, Maja D. and Erić-Nikolić, Aleksandra and Kolundžija, Branka and Hamel, Ernest and Ristić, Slavica S. and Juranić, Ivan and Drakulić, Branko",
year = "2013",
abstract = "Antiproliferative activity of twenty-nine (E)-4-aryl-4-oxo-2-butenoic acid amides against three human
tumor cell lines (HeLa, FemX, and K562) is reported. Compounds showed antiproliferative activity in
one-digit micromolar to submicromolar concentrations. The most active derivatives toward all the cell
lines tested bear alkyl substituents on the aroyl moiety of the molecules. Fourteen compounds showed
tubulin assembly inhibition at concentrations <20 mM. The most potent inhibitor of tubulin assembly
was unsubstituted compound 1, with IC50 ¼ 2.9 mM. Compound 23 had an oral LD50 in vivo of 45 mg/kg in
mice. Cell cycle analysis on K562 cells showed that compounds 1, 2 and 23 caused accumulation of cells
in the G2/M phase, but inhibition of microtubule polymerization is not the principal mode of action of
the compounds. Nevertheless, they may be useful leads for the design of a new class of antitubulin
agents.",
publisher = "Elsevier Masson SAS.",
journal = "European Journal of Medicinal Chemistry",
title = "(E)-4-Aryl-4-oxo-2-butenoic acid amides, chalconeearoylacrylic acid chimeras: Design, antiproliferative activity and inhibition of tubulin polymerization",
volume = "62",
pages = "40-50",
doi = "10.1016/j.ejmech.2013.01.006"
}

Vitorović-Todorović, M. D., Erić-Nikolić, A., Kolundžija, B., Hamel, E., Ristić, S. S., Juranić, I.,& Drakulić, B.. (2013). (E)-4-Aryl-4-oxo-2-butenoic acid amides, chalconeearoylacrylic acid chimeras: Design, antiproliferative activity and inhibition of tubulin polymerization. in European Journal of Medicinal Chemistry
Elsevier Masson SAS.., 62, 40-50.
https://doi.org/10.1016/j.ejmech.2013.01.006

Vitorović-Todorović MD, Erić-Nikolić A, Kolundžija B, Hamel E, Ristić SS, Juranić I, Drakulić B. (E)-4-Aryl-4-oxo-2-butenoic acid amides, chalconeearoylacrylic acid chimeras: Design, antiproliferative activity and inhibition of tubulin polymerization. in European Journal of Medicinal Chemistry. 2013;62:40-50.
doi:10.1016/j.ejmech.2013.01.006 .

Vitorović-Todorović, Maja D., Erić-Nikolić, Aleksandra, Kolundžija, Branka, Hamel, Ernest, Ristić, Slavica S., Juranić, Ivan, Drakulić, Branko, "(E)-4-Aryl-4-oxo-2-butenoic acid amides, chalconeearoylacrylic acid chimeras: Design, antiproliferative activity and inhibition of tubulin polymerization" in European Journal of Medicinal Chemistry, 62 (2013):40-50,
https://doi.org/10.1016/j.ejmech.2013.01.006 . .