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
Schematic representation of mechanism of action of HHyPyPyrd on cancer cell proliferation. [Display omitted] 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...
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Published in: | Results in Chemistry Vol. 3; p. 100104 |
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01-01-2021
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Abstract | Schematic representation of mechanism of action of HHyPyPyrd on cancer cell proliferation.
[Display omitted]
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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AbstractList | 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. Schematic representation of mechanism of action of HHyPyPyrd on cancer cell proliferation. [Display omitted] 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. |
ArticleNumber | 100104 |
Author | Pokharel, Yuba Raj Pandey, Vivek Yadav, Paras Nath Pokhrel, Prabina Pathak, Ankita Shahi, Nerina Thapa, Ram Sundar |
Author_xml | – sequence: 1 givenname: Nerina surname: Shahi fullname: Shahi, Nerina organization: Faculty of Life Science and Biotechnology, South Asian University, Akbar Bhawan, Chanakyapuri, New Delhi 110021, India – sequence: 2 givenname: Vivek surname: Pandey fullname: Pandey, Vivek organization: Faculty of Life Science and Biotechnology, South Asian University, Akbar Bhawan, Chanakyapuri, New Delhi 110021, India – sequence: 3 givenname: Ankita surname: Pathak fullname: Pathak, Ankita organization: Pharmaceutical Chemistry, SPER, Jamia Hamdard University, Hamdard Nagar, New Delhi, India – sequence: 4 givenname: Ram Sundar surname: Thapa fullname: Thapa, Ram Sundar organization: Central Department of Chemistry, Tribhuvan University, Kirtipur, Kathmandu, Nepal – sequence: 5 givenname: Prabina surname: Pokhrel fullname: Pokhrel, Prabina organization: Central Department of Chemistry, Tribhuvan University, Kirtipur, Kathmandu, Nepal – sequence: 6 givenname: Yuba Raj surname: Pokharel fullname: Pokharel, Yuba Raj email: yrp@sau.ac.in organization: Faculty of Life Science and Biotechnology, South Asian University, Akbar Bhawan, Chanakyapuri, New Delhi 110021, India – sequence: 7 givenname: Paras Nath surname: Yadav fullname: Yadav, Paras Nath email: paras.yadav@tu.edu.np organization: Central Department of Chemistry, Tribhuvan University, Kirtipur, Kathmandu, Nepal |
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CitedBy_id | crossref_primary_10_1016_j_molstruc_2023_136945 crossref_primary_10_1016_j_poly_2024_116949 crossref_primary_10_1016_j_molstruc_2022_134549 crossref_primary_10_1021_acsomega_3c03824 |
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Keywords | 3-Hydroxypyridine Anti-cancer activities ESI-mass spectrometry Thiosemicarbazone ZN(II) complexes MAPK signaling pathway |
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Zinc(II) complexes of 3-hydroxy-2-formylpyridine... Zinc(II) complexes of 3-hydroxy-2-formylpyridine N(4)-methylthiosemicarbazone (1) and 3-hydroxy-2-formylpyridine N(4)-pyrrolidinyl thiosemicarbazone (2)... |
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SubjectTerms | 3-Hydroxypyridine Anti-cancer activities ESI-mass spectrometry MAPK signaling pathway Thiosemicarbazone ZN(II) complexes |
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 |
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