Synthesis, biological evaluation and computer-aided discovery of new thiazolidine-2,4-dione derivatives as potential antitumor VEGFR-2 inhibitors.

ABSTRACT: In this study, novel VEGFR-2-targeting thiazolidine-2,4-dione derivatives with potential anticancer properties were designed and synthesized. The ability of the designed derivatives to inhibit VEGFR-2 and stop the growth of three different cancer cell types (HT-29, A-549, and HCT-116) was examined in vitro. The IC₅₀ value of compound 15, 0.081 μM, demonstrated the best anti-VEGFR-2 potency. Additionally, compound 15 showed remarkable anti-proliferative activities against the tested cancer cell lines, with IC₅₀ values ranging from 13.56 to 17.8 μM. Additional flow cytometric investigations showed that compound 15 increased apoptosis in HT-29 cancer cells (from 3.1% to 31.4%) arresting their growth in the S phase. Furthermore, compound 15's apoptosis induction in

SUBMITTER: Elkady H 

PROVIDER: S-EPMC10508263 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature