Development of Coumarin-Based Hydroxamates as Histone Deacetylase Inhibitors with Antitumor Activities.

ABSTRACT: Histone deacetylases (HDACs) have been proved to be promising targets for the treatment of cancer, and five histone deacetylase inhibitors (HDACis) have been approved on the market for the treatment of different lymphomas. In our previous work, we designed a series of novel coumarin-containing hydroxamate HDACis, among which compounds 6 and 7 displayed promising activities against tumor growth. Based on a molecular docking study, we further developed 26 additional analogues with the aim to improve activity of designed compounds. Several of these new derivatives not only showed excellent HDAC1 inhibitory effects, but also displayed significant growth inhibitory activities against four human cancer cell lines. Representative compounds, 13a and 13c, showed potent a

SUBMITTER: Zhao N 

PROVIDER: S-EPMC7036849 | biostudies-literature | 2020 Feb

REPOSITORIES: biostudies-literature