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Quinoline based mono- and bis-(thio) carbohydrazones: synthesis, anticancer activity in 2D and 3D cancer and cancer stem cell models

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2016
1893.pdf (3.424Mb)
Authors
Božić, Aleksandra R.
Marinković, Aleksandar D.
Bjelogrlić, Snežana K.
Todorović, Tamara
Cvijetić, Ilija
Novaković, Irena
Muller, Christian D.
Filipovic, Nenad R.
Article (Published version)
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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.

Source:
RSC Advances, 2016, 6, 106, 104763-104781
Publisher:
  • Royal Soc Chemistry, Cambridge
Funding / projects:
  • Interactions of natural products, their derivatives and coordination compounds with proteins and nucleic acids (RS-172055)
  • Study of the Synthesis, Structure and Activity of Natural and Synthetic Organic Compounds (RS-172013)
  • COST Action CM1106 StemChem - "Chemical Approaches to Targeting Drug Resistance in Cancer Stem Cells"

DOI: 10.1039/c6ra23940d

ISSN: 2046-2069

WoS: 000388111900107

Scopus: 2-s2.0-84994477669
[ Google Scholar ]
22
14
URI
https://cer.ihtm.bg.ac.rs/handle/123456789/1895
Collections
  • Radovi istraživača / Researchers' publications
Institution/Community
IHTM
TY  - JOUR
AU  - Božić, Aleksandra R.
AU  - Marinković, Aleksandar D.
AU  - Bjelogrlić, Snežana K.
AU  - Todorović, Tamara
AU  - Cvijetić, Ilija
AU  - Novaković, Irena
AU  - Muller, Christian D.
AU  - Filipovic, Nenad R.
PY  - 2016
UR  - https://cer.ihtm.bg.ac.rs/handle/123456789/1895
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
VL  - 6
IS  - 106
SP  - 104763
EP  - 104781
DO  - 10.1039/c6ra23940d
ER  - 
@article{
author = "Božić, Aleksandra R. and Marinković, Aleksandar D. and Bjelogrlić, Snežana K. and Todorović, Tamara and Cvijetić, Ilija and Novaković, Irena and Muller, Christian D. and Filipovic, Nenad R.",
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",
volume = "6",
number = "106",
pages = "104763-104781",
doi = "10.1039/c6ra23940d"
}
Božić, A. R., Marinković, A. D., Bjelogrlić, S. K., Todorović, T., Cvijetić, I., Novaković, I., Muller, C. D.,& Filipovic, N. R.. (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 AR, Marinković AD, Bjelogrlić SK, Todorović T, Cvijetić I, Novaković I, Muller CD, Filipovic NR. 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 R., Marinković, Aleksandar D., Bjelogrlić, Snežana K., Todorović, Tamara, Cvijetić, Ilija, Novaković, Irena, Muller, Christian D., Filipovic, Nenad R., "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 . .

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