Akçok, İsmailMete, DeryaŞen, AyhanKasaplar, PınarKorkmaz, Kemal S.Çağır, Ali2017-10-172017-10-172017Akçok, İ., Mete, D., Şen, A., Kasaplar, P., Korkmaz, K. S., and Çağır, A. (2017). Synthesis and Topoisomerase I inhibitory properties of klavuzon derivatives. Bioorganic Chemistry, 71, 275-284. doi:10.1016/j.bioorg.2017.02.0120045-20680045-2068http://doi.org/10.1016/j.bioorg.2017.02.012https://hdl.handle.net/11147/6369Klavuzon is a naphthalen-1-yl substituted α,β-unsaturated δ-lactone derivative, and is one of the anti-proliferative members of this class of compounds. Asymmetric and racemic syntheses of novel α,β-unsaturated δ-lactone derivatives are important to investigate their potential for the treatment of cancer. In this study, asymmetric and racemic syntheses of heteroatom-substituted klavuzon derivatives are reported. The syntheses were completed by a well-known three-step procedure. Anti-proliferative activity of seven novel racemic klavuzon derivatives were reported against MCF-7, PC3, HCT116 p53+/+ and HCT116 p53−/− cancer cell lines. Topoisomerase I inhibitory properties of 5,6-dihydro-2H-pyran-2-one derivatives were also studied. © 2017 Elsevier Inc.eninfo:eu-repo/semantics/openAccessKlavuzonTopoisomerase I inhibitionAnti-proliferative activityLactonesArticle2-s2.0-8501363840510.1016/j.bioorg.2017.02.01210.1016/j.bioorg.2017.02.012