Anticancer potential of 3-hydroxypyridine-2-carboxaldehyde N(4)-methyl and pyrrolidinylthiosemicarbazones and their Zn(II) complexes in different cancers via targeting MAPK superfamily signaling pathway

Zinc(II) complexes of 3-hydroxy-2-formylpyridine N(4)-methylthiosemicarbazone (1) and 3-hydroxy-2-formylpyridine N(4)-pyrrolidinyl thiosemicarbazone (2) respectively have been synthesized and characterized by elemental analysis, IR, UV–Vis, 1H NMR spectroscopy and mass spectrometry. These compounds...

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Main Authors: Nerina Shahi, Vivek Pandey, Ankita Pathak, Ram Sundar Thapa, Prabina Pokhrel, Yuba Raj Pokharel, Paras Nath Yadav
Format: Article
Language:English
Published: Elsevier 2021-01-01
Series:Results in Chemistry
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Online Access:http://www.sciencedirect.com/science/article/pii/S2211715621000096
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author Nerina Shahi
Vivek Pandey
Ankita Pathak
Ram Sundar Thapa
Prabina Pokhrel
Yuba Raj Pokharel
Paras Nath Yadav
author_facet Nerina Shahi
Vivek Pandey
Ankita Pathak
Ram Sundar Thapa
Prabina Pokhrel
Yuba Raj Pokharel
Paras Nath Yadav
author_sort Nerina Shahi
collection DOAJ
description Zinc(II) complexes of 3-hydroxy-2-formylpyridine N(4)-methylthiosemicarbazone (1) and 3-hydroxy-2-formylpyridine N(4)-pyrrolidinyl thiosemicarbazone (2) respectively have been synthesized and characterized by elemental analysis, IR, UV–Vis, 1H NMR spectroscopy and mass spectrometry. These compounds were investigated for their antiproliferative potential against PC3 (Prostate Cancer), DU145 (Prostate Cancer), A549 (Lung Cancer), A431 (skin cancer) and Hela (Cervical Cancer cell) cell lines. All the compounds showed good antiproliferative activity against the tested cell lines. However, compound HHyPyPyrd showed remarkable antiproliferative activity against PC3 cell line with an IC50 of 0.69 µM. Cell death analysis by propidium iodide staining showed significant increase in cell death of PC3 cells in a concentration dependent manner. Furthermore, cell cycle analysis showed cell cycle arrest of PC3 cells at S phase. Our study shows that compound HHyPyPyrd induces the downregulation of JNK, c-Jun and Erk.
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spelling doaj.art-5e75144bd8d4467c9f2516d2b28c8a362022-12-21T19:21:14ZengElsevierResults in Chemistry2211-71562021-01-013100104Anticancer potential of 3-hydroxypyridine-2-carboxaldehyde N(4)-methyl and pyrrolidinylthiosemicarbazones and their Zn(II) complexes in different cancers via targeting MAPK superfamily signaling pathwayNerina Shahi0Vivek Pandey1Ankita Pathak2Ram Sundar Thapa3Prabina Pokhrel4Yuba Raj Pokharel5Paras Nath Yadav6Faculty of Life Science and Biotechnology, South Asian University, Akbar Bhawan, Chanakyapuri, New Delhi 110021, IndiaFaculty of Life Science and Biotechnology, South Asian University, Akbar Bhawan, Chanakyapuri, New Delhi 110021, IndiaPharmaceutical Chemistry, SPER, Jamia Hamdard University, Hamdard Nagar, New Delhi, IndiaCentral Department of Chemistry, Tribhuvan University, Kirtipur, Kathmandu, NepalCentral Department of Chemistry, Tribhuvan University, Kirtipur, Kathmandu, NepalFaculty of Life Science and Biotechnology, South Asian University, Akbar Bhawan, Chanakyapuri, New Delhi 110021, India; Corresponding authors.Central Department of Chemistry, Tribhuvan University, Kirtipur, Kathmandu, Nepal; Corresponding authors.Zinc(II) complexes of 3-hydroxy-2-formylpyridine N(4)-methylthiosemicarbazone (1) and 3-hydroxy-2-formylpyridine N(4)-pyrrolidinyl thiosemicarbazone (2) respectively have been synthesized and characterized by elemental analysis, IR, UV–Vis, 1H NMR spectroscopy and mass spectrometry. These compounds were investigated for their antiproliferative potential against PC3 (Prostate Cancer), DU145 (Prostate Cancer), A549 (Lung Cancer), A431 (skin cancer) and Hela (Cervical Cancer cell) cell lines. All the compounds showed good antiproliferative activity against the tested cell lines. However, compound HHyPyPyrd showed remarkable antiproliferative activity against PC3 cell line with an IC50 of 0.69 µM. Cell death analysis by propidium iodide staining showed significant increase in cell death of PC3 cells in a concentration dependent manner. Furthermore, cell cycle analysis showed cell cycle arrest of PC3 cells at S phase. Our study shows that compound HHyPyPyrd induces the downregulation of JNK, c-Jun and Erk.http://www.sciencedirect.com/science/article/pii/S2211715621000096Anti-cancer activitiesESI-mass spectrometry3-HydroxypyridineThiosemicarbazoneZN(II) complexesMAPK signaling pathway
spellingShingle Nerina Shahi
Vivek Pandey
Ankita Pathak
Ram Sundar Thapa
Prabina Pokhrel
Yuba Raj Pokharel
Paras Nath Yadav
Anticancer potential of 3-hydroxypyridine-2-carboxaldehyde N(4)-methyl and pyrrolidinylthiosemicarbazones and their Zn(II) complexes in different cancers via targeting MAPK superfamily signaling pathway
Results in Chemistry
Anti-cancer activities
ESI-mass spectrometry
3-Hydroxypyridine
Thiosemicarbazone
ZN(II) complexes
MAPK signaling pathway
title Anticancer potential of 3-hydroxypyridine-2-carboxaldehyde N(4)-methyl and pyrrolidinylthiosemicarbazones and their Zn(II) complexes in different cancers via targeting MAPK superfamily signaling pathway
title_full Anticancer potential of 3-hydroxypyridine-2-carboxaldehyde N(4)-methyl and pyrrolidinylthiosemicarbazones and their Zn(II) complexes in different cancers via targeting MAPK superfamily signaling pathway
title_fullStr Anticancer potential of 3-hydroxypyridine-2-carboxaldehyde N(4)-methyl and pyrrolidinylthiosemicarbazones and their Zn(II) complexes in different cancers via targeting MAPK superfamily signaling pathway
title_full_unstemmed Anticancer potential of 3-hydroxypyridine-2-carboxaldehyde N(4)-methyl and pyrrolidinylthiosemicarbazones and their Zn(II) complexes in different cancers via targeting MAPK superfamily signaling pathway
title_short Anticancer potential of 3-hydroxypyridine-2-carboxaldehyde N(4)-methyl and pyrrolidinylthiosemicarbazones and their Zn(II) complexes in different cancers via targeting MAPK superfamily signaling pathway
title_sort anticancer potential of 3 hydroxypyridine 2 carboxaldehyde n 4 methyl and pyrrolidinylthiosemicarbazones and their zn ii complexes in different cancers via targeting mapk superfamily signaling pathway
topic Anti-cancer activities
ESI-mass spectrometry
3-Hydroxypyridine
Thiosemicarbazone
ZN(II) complexes
MAPK signaling pathway
url http://www.sciencedirect.com/science/article/pii/S2211715621000096
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