A series of six novel 2-(5-arylidene-2,4-dioxotetrahydrothiazole-3-yl) propanoic acids and six corresponding methyl esters were synthesized. All compounds were characterized by melting points, elemental analysis, FT-IR, H-1 and C-13 NMR spectroscopy. Crystal structure of methyl-2-(5-(4-methoxybenzylidene)-2,4-dioxotetrahydrothiazole-3-yl) propionate was confirmed by X-ray analysis. The antiproliferative activity of all synthesized compounds against human colon cancer, breast cancer and myelogenous leukemia cell lines, i.e. HCT-116, MDA-231 and K562, respectively, was evaluated. The results indicate that antiproliferative activity of the synthesized esters is better than the activity of the corresponding acids. All synthesized compounds showed significant antiproliferative effects against HCT116 cells in all tested concentrations (0.01-100 lM). Moreover, in vitro antimicrobial activity against a wide range of tested microorganisms was examined.
TY - JOUR
AU - Božić, Bojan
AU - Rogan, Jelena
AU - Poleti, Dejan
AU - Rančić, Milica
AU - Trišović, Nemanja
AU - Božić, Biljana
AU - Ušćumlić, Gordana
PY - 2017
UR - http://TechnoRep.tmf.bg.ac.rs/handle/123456789/3607
AB - A series of six novel 2-(5-arylidene-2,4-dioxotetrahydrothiazole-3-yl) propanoic acids and six corresponding methyl esters were synthesized. All compounds were characterized by melting points, elemental analysis, FT-IR, H-1 and C-13 NMR spectroscopy. Crystal structure of methyl-2-(5-(4-methoxybenzylidene)-2,4-dioxotetrahydrothiazole-3-yl) propionate was confirmed by X-ray analysis. The antiproliferative activity of all synthesized compounds against human colon cancer, breast cancer and myelogenous leukemia cell lines, i.e. HCT-116, MDA-231 and K562, respectively, was evaluated. The results indicate that antiproliferative activity of the synthesized esters is better than the activity of the corresponding acids. All synthesized compounds showed significant antiproliferative effects against HCT116 cells in all tested concentrations (0.01-100 lM). Moreover, in vitro antimicrobial activity against a wide range of tested microorganisms was examined.
PB - Elsevier Science Bv, Amsterdam
T2 - Arabian Journal of Chemistry
T1 - Synthesis, characterization and biological activity of 2-(5-arylidene-2,4-dioxotetrahydrothiazole-3-yl) propanoic acid derivatives
EP - S2643
SP - S2637
VL - 10
DO - 10.1016/j.arabjc.2013.10.002
ER -
@article{
author = "Božić, Bojan and Rogan, Jelena and Poleti, Dejan and Rančić, Milica and Trišović, Nemanja and Božić, Biljana and Ušćumlić, Gordana",
year = "2017",
abstract = "A series of six novel 2-(5-arylidene-2,4-dioxotetrahydrothiazole-3-yl) propanoic acids and six corresponding methyl esters were synthesized. All compounds were characterized by melting points, elemental analysis, FT-IR, H-1 and C-13 NMR spectroscopy. Crystal structure of methyl-2-(5-(4-methoxybenzylidene)-2,4-dioxotetrahydrothiazole-3-yl) propionate was confirmed by X-ray analysis. The antiproliferative activity of all synthesized compounds against human colon cancer, breast cancer and myelogenous leukemia cell lines, i.e. HCT-116, MDA-231 and K562, respectively, was evaluated. The results indicate that antiproliferative activity of the synthesized esters is better than the activity of the corresponding acids. All synthesized compounds showed significant antiproliferative effects against HCT116 cells in all tested concentrations (0.01-100 lM). Moreover, in vitro antimicrobial activity against a wide range of tested microorganisms was examined.",
publisher = "Elsevier Science Bv, Amsterdam",
journal = "Arabian Journal of Chemistry",
title = "Synthesis, characterization and biological activity of 2-(5-arylidene-2,4-dioxotetrahydrothiazole-3-yl) propanoic acid derivatives",
pages = "S2643-S2637",
volume = "10",
doi = "10.1016/j.arabjc.2013.10.002"
}
Božić, B., Rogan, J., Poleti, D., Rančić, M., Trišović, N., Božić, B.,& Ušćumlić, G.. (2017). Synthesis, characterization and biological activity of 2-(5-arylidene-2,4-dioxotetrahydrothiazole-3-yl) propanoic acid derivatives. in Arabian Journal of Chemistry
Elsevier Science Bv, Amsterdam., 10, S2637-S2643.
https://doi.org/10.1016/j.arabjc.2013.10.002
Božić B, Rogan J, Poleti D, Rančić M, Trišović N, Božić B, Ušćumlić G. Synthesis, characterization and biological activity of 2-(5-arylidene-2,4-dioxotetrahydrothiazole-3-yl) propanoic acid derivatives. in Arabian Journal of Chemistry. 2017;10:S2637-S2643.
doi:10.1016/j.arabjc.2013.10.002 .
Božić, Bojan, Rogan, Jelena, Poleti, Dejan, Rančić, Milica, Trišović, Nemanja, Božić, Biljana, Ušćumlić, Gordana, "Synthesis, characterization and biological activity of 2-(5-arylidene-2,4-dioxotetrahydrothiazole-3-yl) propanoic acid derivatives" in Arabian Journal of Chemistry, 10 (2017):S2637-S2643,
https://doi.org/10.1016/j.arabjc.2013.10.002 . .
