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

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

Turk J Chem

Research Institute for Health Sciences and Technologies (SABITA), Center of Drug Discovery and Development, İstanbul Medipol University, İstanbul, Turkey.

Published: March 2022

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 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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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10395680PMC
http://dx.doi.org/10.55730/1300-0527.3417DOI Listing

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