Synthesis and cytotoxicity evaluation of novel 1,8-acridinedione derivatives bearing phthalimide moiety as potential antitumor agents.

ABSTRACT: In this study, we aimed to develop hybrid antitumor compounds by synthesizing and characterizing novel N-substituted acrididine-1,8-dione derivatives, designed as hybrids of phthalimide and acridine-1,8-diones. We employed a three-step synthetic strategy and characterized all compounds using IR, ¹H NMR, ¹³C NMR, and LC-MS. The cytotoxicity and antitumor activity of five compounds (8c, 8f, 8h, 8i, and 8L) against four cancer cell lines (H460, A431, A549, and MDA-MB-231) compared to human skin fibroblast cells were evaluated. Among the synthesized compounds, compound 8f showed promising activity against skin and lung cancers, with favorable IC₅₀ values and selectivity index. The relative changes in mRNA expression levels of four key genes (p53, TOP2B, p38, an

SUBMITTER: Khatab HA 

PROVIDER: S-EPMC10497682 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature