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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...

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Autores principales: 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.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
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.
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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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