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

Bilgesu Onur Sucu; Elif Beyza Koç

doi:10.55730/1300-0527.3417

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

Turk J Chem. 2022 Mar 12;46(4):1089-1096. doi: 10.55730/1300-0527.3417. eCollection 2022.

Authors

Bilgesu Onur Sucu^{1

2}, Elif Beyza Koç¹

Affiliations

¹ Research Institute for Health Sciences and Technologies (SABITA), Center of Drug Discovery and Development, İstanbul Medipol University, İstanbul, Turkey.
² Department of Medical Services and Techniques, Vocational School of Health Services, İstanbul Medipol University, İstanbul, Turkey.

Abstract

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 IC₅₀ 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.

Keywords: 1; 2; 3; 4-Oxadiazoles; anticancer activity; glioblastoma cancer cells.

Grants and funding

We thank the Scientific and Technological Research Council of Turkey (TÜBİTAK) for its financial support (project no:119Z116).