Synthesis, Labeling and Biological Evolution of New Thiopyrano[2,3-b]pyridine Derivatives as Potential Anticancer Agents

The new thiopyrano[2,3-b]pyridines 4–9 could be synthesized from the nicotinonitrile derivative 1. The cytotoxicity activity of the selected compounds 5, 6 and 8 was tested against MCF-7 and HCT-116 cell lines. The compound 5 (TP5) exhibited significant inhibitory activity and displayed the most pot...

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Main Authors: Mamdouh Sofan, Wafaa Hamama, Ibrahim Ibrahim EL-Hawary, Ismail Taha Ibrahim, Hanafi Hassan Zoorob
Format: Article
Language:English
Published: Slovenian Chemical Society 2019-09-01
Series:Acta Chimica Slovenica
Subjects:
Online Access:https://journals.matheo.si/index.php/ACSi/article/view/4980
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author Mamdouh Sofan
Wafaa Hamama
Ibrahim Ibrahim EL-Hawary
Ismail Taha Ibrahim
Hanafi Hassan Zoorob
author_facet Mamdouh Sofan
Wafaa Hamama
Ibrahim Ibrahim EL-Hawary
Ismail Taha Ibrahim
Hanafi Hassan Zoorob
author_sort Mamdouh Sofan
collection DOAJ
description The new thiopyrano[2,3-b]pyridines 4–9 could be synthesized from the nicotinonitrile derivative 1. The cytotoxicity activity of the selected compounds 5, 6 and 8 was tested against MCF-7 and HCT-116 cell lines. The compound 5 (TP5) exhibited significant inhibitory activity and displayed the most potent activity, more than 6 and 8. The compound 5 with potent inhibitory activity in tumor growth inhibition would be a potential anticancer agent. In the light of this result, the labeled 125I-compound 5 (125I-TP5) was prepared and its cytotoxicity against ascites tumor in mice has been evaluated. The results show that compound 5 (TP5) may be potentially used as a radiopharmaceutical for tumor diagnosis when labeled with 125I.
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spelling doaj.art-768b20b8657d4e86ac41452aaba285bf2022-12-22T03:16:10ZengSlovenian Chemical SocietyActa Chimica Slovenica1318-02071580-31552019-09-0166359260210.17344/acsi.2019.4980730Synthesis, Labeling and Biological Evolution of New Thiopyrano[2,3-b]pyridine Derivatives as Potential Anticancer AgentsMamdouh Sofan0Wafaa Hamama1Ibrahim Ibrahim EL-Hawary2Ismail Taha Ibrahim3Hanafi Hassan Zoorob4Department of Chemistry, Faculty of Science, Damietta University, New Damietta 34517, EgyptChemistry Department, Faculty of Science, Mansoura University, EgyptChemistry Department, Faculty of Science, Damietta University, EgyptHot Laboratories Center, Atomic Energy Authority, Cairo, EgyptChemistry Department, Faculty of Science, Mansoura University, EgyptThe new thiopyrano[2,3-b]pyridines 4–9 could be synthesized from the nicotinonitrile derivative 1. The cytotoxicity activity of the selected compounds 5, 6 and 8 was tested against MCF-7 and HCT-116 cell lines. The compound 5 (TP5) exhibited significant inhibitory activity and displayed the most potent activity, more than 6 and 8. The compound 5 with potent inhibitory activity in tumor growth inhibition would be a potential anticancer agent. In the light of this result, the labeled 125I-compound 5 (125I-TP5) was prepared and its cytotoxicity against ascites tumor in mice has been evaluated. The results show that compound 5 (TP5) may be potentially used as a radiopharmaceutical for tumor diagnosis when labeled with 125I.https://journals.matheo.si/index.php/ACSi/article/view/4980Nicotinonitrilethiopyrano[2,3-b]pyridinecytototoxic activityascites tumor
spellingShingle Mamdouh Sofan
Wafaa Hamama
Ibrahim Ibrahim EL-Hawary
Ismail Taha Ibrahim
Hanafi Hassan Zoorob
Synthesis, Labeling and Biological Evolution of New Thiopyrano[2,3-b]pyridine Derivatives as Potential Anticancer Agents
Acta Chimica Slovenica
Nicotinonitrile
thiopyrano[2,3-b]pyridine
cytototoxic activity
ascites tumor
title Synthesis, Labeling and Biological Evolution of New Thiopyrano[2,3-b]pyridine Derivatives as Potential Anticancer Agents
title_full Synthesis, Labeling and Biological Evolution of New Thiopyrano[2,3-b]pyridine Derivatives as Potential Anticancer Agents
title_fullStr Synthesis, Labeling and Biological Evolution of New Thiopyrano[2,3-b]pyridine Derivatives as Potential Anticancer Agents
title_full_unstemmed Synthesis, Labeling and Biological Evolution of New Thiopyrano[2,3-b]pyridine Derivatives as Potential Anticancer Agents
title_short Synthesis, Labeling and Biological Evolution of New Thiopyrano[2,3-b]pyridine Derivatives as Potential Anticancer Agents
title_sort synthesis labeling and biological evolution of new thiopyrano 2 3 b pyridine derivatives as potential anticancer agents
topic Nicotinonitrile
thiopyrano[2,3-b]pyridine
cytototoxic activity
ascites tumor
url https://journals.matheo.si/index.php/ACSi/article/view/4980
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