Novel Canthin-6-one Derivatives: Design, Synthesis, and Their Antiproliferative Activities via Inducing Apoptosis, Deoxyribonucleic Acid Damage, and Ferroptosis.

ABSTRACT: A series of novel canthin-6-one (CO) derivatives (8a-l) were designed and synthesized by introducing different amide side chains at the C-2 position, and their water solubility, antiproliferative activity, and preliminary mechanism were investigated. Most compounds displayed high cytotoxicity exhibiting low-micromolar IC₅₀ values against four human cancer cell lines, especially HT29 cells. Meanwhile, the water solubility of active CO derivatives was significantly improved. Among these compounds, compound 8h with the N-methyl piperazine group exhibiting the highest antiproliferative capability with an IC₅₀ value of 1.0 μM against HT29 cells, which was 8.6-fold lower than that of CO. Furthermore, 8h could upregulate the levels of reactive oxy

SUBMITTER: Ding J 

PROVIDER: S-EPMC10468838 | biostudies-literature | 2023 Aug

REPOSITORIES: biostudies-literature