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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Elsevier
2021-01-01
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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. |
first_indexed | 2024-12-21T00:58:12Z |
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id | doaj.art-5e75144bd8d4467c9f2516d2b28c8a36 |
institution | Directory Open Access Journal |
issn | 2211-7156 |
language | English |
last_indexed | 2024-12-21T00:58:12Z |
publishDate | 2021-01-01 |
publisher | Elsevier |
record_format | Article |
series | Results in Chemistry |
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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