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Antiproliferative Activity of Some Newly Synthesized Substituted Nicotinamides Candidates Using Pyridine-2(1H) thione Derivatives as Synthon
[Image: see text] Some new pyridinethione and thienopyridine derivatives have been synthesized and evaluated for their antiproliferative activity using the MTT assay. Nicotinamide derivatives 3 have been synthesized and used for the preparation of new condensed thieno [2,3-b]pyridines by their react...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical Society
2022
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8973085/ https://www.ncbi.nlm.nih.gov/pubmed/35382307 http://dx.doi.org/10.1021/acsomega.1c06951 |
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author | Elnaggar, Dina H. Mohamed, Ashraf M. Abdel Hafez, Naglaa A. Azab, Mohamed E. Elasasy, Manar E. A. Awad, Hanem M. Farghaly, Thoraya A. Amr, Abd El-Galil E. |
author_facet | Elnaggar, Dina H. Mohamed, Ashraf M. Abdel Hafez, Naglaa A. Azab, Mohamed E. Elasasy, Manar E. A. Awad, Hanem M. Farghaly, Thoraya A. Amr, Abd El-Galil E. |
author_sort | Elnaggar, Dina H. |
collection | PubMed |
description | [Image: see text] Some new pyridinethione and thienopyridine derivatives have been synthesized and evaluated for their antiproliferative activity using the MTT assay. Nicotinamide derivatives 3 have been synthesized and used for the preparation of new condensed thieno [2,3-b]pyridines by their reactions with active halo compounds. Finally the synthesized thienopyridine underwent ring closure whenever possible through boiling in a solution of sodium ethoxide. The antiproliferative evaluation against (HCT-116, HepG-2, and MCF-7) human cancer cells and one human healthy cell line (BJ-1) revealed that compounds 3b, 4c–5d, 7b–12a, 10d, and 13b have interesting antitumor activity specifically as antihepatocellular and anticolon cellular carcinoma agents. Besides, the docking results for most active derivatives were in agreement with the in vitro antitumor results. |
format | Online Article Text |
id | pubmed-8973085 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | American Chemical Society |
record_format | MEDLINE/PubMed |
spelling | pubmed-89730852022-04-04 Antiproliferative Activity of Some Newly Synthesized Substituted Nicotinamides Candidates Using Pyridine-2(1H) thione Derivatives as Synthon Elnaggar, Dina H. Mohamed, Ashraf M. Abdel Hafez, Naglaa A. Azab, Mohamed E. Elasasy, Manar E. A. Awad, Hanem M. Farghaly, Thoraya A. Amr, Abd El-Galil E. ACS Omega [Image: see text] Some new pyridinethione and thienopyridine derivatives have been synthesized and evaluated for their antiproliferative activity using the MTT assay. Nicotinamide derivatives 3 have been synthesized and used for the preparation of new condensed thieno [2,3-b]pyridines by their reactions with active halo compounds. Finally the synthesized thienopyridine underwent ring closure whenever possible through boiling in a solution of sodium ethoxide. The antiproliferative evaluation against (HCT-116, HepG-2, and MCF-7) human cancer cells and one human healthy cell line (BJ-1) revealed that compounds 3b, 4c–5d, 7b–12a, 10d, and 13b have interesting antitumor activity specifically as antihepatocellular and anticolon cellular carcinoma agents. Besides, the docking results for most active derivatives were in agreement with the in vitro antitumor results. American Chemical Society 2022-03-16 /pmc/articles/PMC8973085/ /pubmed/35382307 http://dx.doi.org/10.1021/acsomega.1c06951 Text en © 2022 The Authors. Published by American Chemical Society https://creativecommons.org/licenses/by-nc-nd/4.0/Permits non-commercial access and re-use, provided that author attribution and integrity are maintained; but does not permit creation of adaptations or other derivative works (https://creativecommons.org/licenses/by-nc-nd/4.0/). |
spellingShingle | Elnaggar, Dina H. Mohamed, Ashraf M. Abdel Hafez, Naglaa A. Azab, Mohamed E. Elasasy, Manar E. A. Awad, Hanem M. Farghaly, Thoraya A. Amr, Abd El-Galil E. Antiproliferative Activity of Some Newly Synthesized Substituted Nicotinamides Candidates Using Pyridine-2(1H) thione Derivatives as Synthon |
title | Antiproliferative Activity of Some Newly Synthesized
Substituted Nicotinamides Candidates Using Pyridine-2(1H) thione Derivatives as Synthon |
title_full | Antiproliferative Activity of Some Newly Synthesized
Substituted Nicotinamides Candidates Using Pyridine-2(1H) thione Derivatives as Synthon |
title_fullStr | Antiproliferative Activity of Some Newly Synthesized
Substituted Nicotinamides Candidates Using Pyridine-2(1H) thione Derivatives as Synthon |
title_full_unstemmed | Antiproliferative Activity of Some Newly Synthesized
Substituted Nicotinamides Candidates Using Pyridine-2(1H) thione Derivatives as Synthon |
title_short | Antiproliferative Activity of Some Newly Synthesized
Substituted Nicotinamides Candidates Using Pyridine-2(1H) thione Derivatives as Synthon |
title_sort | antiproliferative activity of some newly synthesized
substituted nicotinamides candidates using pyridine-2(1h) thione derivatives as synthon |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8973085/ https://www.ncbi.nlm.nih.gov/pubmed/35382307 http://dx.doi.org/10.1021/acsomega.1c06951 |
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