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Synthesis of novel oxadiazole derivatives and their cytotoxic activity against various cancer cell lines

Caffeic acid (CA), ferulic acid (FA) and caffeic acid phenethyl ester (CAPE) have a broad anticancer effect on various cell lines. In this study, nine ferulic and caffeic acid-based 1,2,4 and 1,3,4 oxadiazole molecular hybrids were synthesized and their cytotoxic activity was evaluated mainly agains...

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Autores principales: SUCU, Bilgesu Onur, KOÇ, Elif Beyza
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Scientific and Technological Research Council of Turkey (TUBITAK) 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10395680/
https://www.ncbi.nlm.nih.gov/pubmed/37538768
http://dx.doi.org/10.55730/1300-0527.3417
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author SUCU, Bilgesu Onur
KOÇ, Elif Beyza
author_facet SUCU, Bilgesu Onur
KOÇ, Elif Beyza
author_sort SUCU, Bilgesu Onur
collection PubMed
description Caffeic acid (CA), ferulic acid (FA) and caffeic acid phenethyl ester (CAPE) have a broad anticancer effect on various cell lines. In this study, nine ferulic and caffeic acid-based 1,2,4 and 1,3,4 oxadiazole molecular hybrids were synthesized and their cytotoxic activity was evaluated mainly against Glioblastoma (GBM) cell lines. Compounds 1 and 5 exhibited the highest inhibitory activity against three different GBM cell lines (LN229, T98G, and U87), without toxicity to healthy human mesenchymal stem cells (hMSC). In addition, their cytotoxicity was also evaluated against three additional cancer cell lines and more inhibitory results were found than GBM cell lines. The IC(50) values of compound 5 in U87, T98G, LN229, SKOV3, MCF7, and A549 cells were determined as 35.1, 34.4, 37.9, 14.2, 30.9, and 18.3 μM. In the light of biological activity studies, the developed compounds have a high potential to lead studies for the development of new drug candidates for the treatment of cancer.
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spelling pubmed-103956802023-08-03 Synthesis of novel oxadiazole derivatives and their cytotoxic activity against various cancer cell lines SUCU, Bilgesu Onur KOÇ, Elif Beyza Turk J Chem Research Article Caffeic acid (CA), ferulic acid (FA) and caffeic acid phenethyl ester (CAPE) have a broad anticancer effect on various cell lines. In this study, nine ferulic and caffeic acid-based 1,2,4 and 1,3,4 oxadiazole molecular hybrids were synthesized and their cytotoxic activity was evaluated mainly against Glioblastoma (GBM) cell lines. Compounds 1 and 5 exhibited the highest inhibitory activity against three different GBM cell lines (LN229, T98G, and U87), without toxicity to healthy human mesenchymal stem cells (hMSC). In addition, their cytotoxicity was also evaluated against three additional cancer cell lines and more inhibitory results were found than GBM cell lines. The IC(50) values of compound 5 in U87, T98G, LN229, SKOV3, MCF7, and A549 cells were determined as 35.1, 34.4, 37.9, 14.2, 30.9, and 18.3 μM. In the light of biological activity studies, the developed compounds have a high potential to lead studies for the development of new drug candidates for the treatment of cancer. Scientific and Technological Research Council of Turkey (TUBITAK) 2022-03-12 /pmc/articles/PMC10395680/ /pubmed/37538768 http://dx.doi.org/10.55730/1300-0527.3417 Text en © TÜBİTAK https://creativecommons.org/licenses/by/4.0/This work is licensed under a Creative Commons Attribution 4.0 International License.
spellingShingle Research Article
SUCU, Bilgesu Onur
KOÇ, Elif Beyza
Synthesis of novel oxadiazole derivatives and their cytotoxic activity against various cancer cell lines
title Synthesis of novel oxadiazole derivatives and their cytotoxic activity against various cancer cell lines
title_full Synthesis of novel oxadiazole derivatives and their cytotoxic activity against various cancer cell lines
title_fullStr Synthesis of novel oxadiazole derivatives and their cytotoxic activity against various cancer cell lines
title_full_unstemmed Synthesis of novel oxadiazole derivatives and their cytotoxic activity against various cancer cell lines
title_short Synthesis of novel oxadiazole derivatives and their cytotoxic activity against various cancer cell lines
title_sort synthesis of novel oxadiazole derivatives and their cytotoxic activity against various cancer cell lines
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10395680/
https://www.ncbi.nlm.nih.gov/pubmed/37538768
http://dx.doi.org/10.55730/1300-0527.3417
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