A comparative study of antitumor activity of mono- and bis-quinoline based (thio) carbohydrazones was investigated by a series of tests on two human malignant cell lines: acute monocytic leukemia (THP-1) and pancreatic adenocarcinoma cancer stem cells (AsPC-1). Thiocarbohydrazones (TCHs) revealed superior pro-apoptotic activity over carbohydrazones (CHs) on both tested cell phenotypes, also displaying multi-target profile activities. Programmed cell death triggered by TCHs was partially caspase-dependent, mainly caspase-8 related. Activity against cancer stem cells (CSCs) was evaluated on 2D monolayers and 3D spheroidal models, where two out of three tested bis-TCHs successfully stimulated apoptosis accompanied by a reduction in size of treated spheres. Additionally, all bis-TCHs induced significant decrease in percentage of CD44-expressing AsPC-1 cells that indicate on their ability to induce reprogramming of CSC phenotype. Current results highly support further assessment of bis-TCHs... in order to specify their specific targets in cancer cells and particularly in the CSCs subpopulation.
Source:
RSC Advances, 2016, 6, 106, 104763-104781
Publisher:
Royal Soc Chemistry, Cambridge
Funding / projects:
COST Action CM1106 StemChem - "Chemical Approaches to Targeting Drug Resistance in Cancer Stem Cells"
TY - JOUR
AU - Božić, Aleksandra
AU - Marinković, Aleksandar
AU - Bjelogrlić, Snežana
AU - Todorović, Tamara R.
AU - Cvijetić, Ilija N.
AU - Novaković, Irena
AU - Muller, Christian D.
AU - Filipović, Nenad
PY - 2016
UR - http://aspace.agrif.bg.ac.rs/handle/123456789/4065
AB - A comparative study of antitumor activity of mono- and bis-quinoline based (thio) carbohydrazones was investigated by a series of tests on two human malignant cell lines: acute monocytic leukemia (THP-1) and pancreatic adenocarcinoma cancer stem cells (AsPC-1). Thiocarbohydrazones (TCHs) revealed superior pro-apoptotic activity over carbohydrazones (CHs) on both tested cell phenotypes, also displaying multi-target profile activities. Programmed cell death triggered by TCHs was partially caspase-dependent, mainly caspase-8 related. Activity against cancer stem cells (CSCs) was evaluated on 2D monolayers and 3D spheroidal models, where two out of three tested bis-TCHs successfully stimulated apoptosis accompanied by a reduction in size of treated spheres. Additionally, all bis-TCHs induced significant decrease in percentage of CD44-expressing AsPC-1 cells that indicate on their ability to induce reprogramming of CSC phenotype. Current results highly support further assessment of bis-TCHs in order to specify their specific targets in cancer cells and particularly in the CSCs subpopulation.
PB - Royal Soc Chemistry, Cambridge
T2 - RSC Advances
T1 - Quinoline based mono- and bis-(thio) carbohydrazones: synthesis, anticancer activity in 2D and 3D cancer and cancer stem cell models
EP - 104781
IS - 106
SP - 104763
VL - 6
DO - 10.1039/c6ra23940d
ER -
@article{
author = "Božić, Aleksandra and Marinković, Aleksandar and Bjelogrlić, Snežana and Todorović, Tamara R. and Cvijetić, Ilija N. and Novaković, Irena and Muller, Christian D. and Filipović, Nenad",
year = "2016",
abstract = "A comparative study of antitumor activity of mono- and bis-quinoline based (thio) carbohydrazones was investigated by a series of tests on two human malignant cell lines: acute monocytic leukemia (THP-1) and pancreatic adenocarcinoma cancer stem cells (AsPC-1). Thiocarbohydrazones (TCHs) revealed superior pro-apoptotic activity over carbohydrazones (CHs) on both tested cell phenotypes, also displaying multi-target profile activities. Programmed cell death triggered by TCHs was partially caspase-dependent, mainly caspase-8 related. Activity against cancer stem cells (CSCs) was evaluated on 2D monolayers and 3D spheroidal models, where two out of three tested bis-TCHs successfully stimulated apoptosis accompanied by a reduction in size of treated spheres. Additionally, all bis-TCHs induced significant decrease in percentage of CD44-expressing AsPC-1 cells that indicate on their ability to induce reprogramming of CSC phenotype. Current results highly support further assessment of bis-TCHs in order to specify their specific targets in cancer cells and particularly in the CSCs subpopulation.",
publisher = "Royal Soc Chemistry, Cambridge",
journal = "RSC Advances",
title = "Quinoline based mono- and bis-(thio) carbohydrazones: synthesis, anticancer activity in 2D and 3D cancer and cancer stem cell models",
pages = "104781-104763",
number = "106",
volume = "6",
doi = "10.1039/c6ra23940d"
}
Božić, A., Marinković, A., Bjelogrlić, S., Todorović, T. R., Cvijetić, I. N., Novaković, I., Muller, C. D.,& Filipović, N.. (2016). Quinoline based mono- and bis-(thio) carbohydrazones: synthesis, anticancer activity in 2D and 3D cancer and cancer stem cell models. in RSC Advances
Royal Soc Chemistry, Cambridge., 6(106), 104763-104781.
https://doi.org/10.1039/c6ra23940d
Božić A, Marinković A, Bjelogrlić S, Todorović TR, Cvijetić IN, Novaković I, Muller CD, Filipović N. Quinoline based mono- and bis-(thio) carbohydrazones: synthesis, anticancer activity in 2D and 3D cancer and cancer stem cell models. in RSC Advances. 2016;6(106):104763-104781.
doi:10.1039/c6ra23940d .
Božić, Aleksandra, Marinković, Aleksandar, Bjelogrlić, Snežana, Todorović, Tamara R., Cvijetić, Ilija N., Novaković, Irena, Muller, Christian D., Filipović, Nenad, "Quinoline based mono- and bis-(thio) carbohydrazones: synthesis, anticancer activity in 2D and 3D cancer and cancer stem cell models" in RSC Advances, 6, no. 106 (2016):104763-104781,
https://doi.org/10.1039/c6ra23940d . .
