Inhibitory Effects of B-, C-, and E-Ring-Truncated Deguelin Derivatives Against A549, HCT116, and MCF-7 Cancer Cells.

ABSTRACT: Deguelin has been extensively studied for its anticancer properties; however, its clinical application has been hindered by concerns about in vivo toxicity. Structural modifications of deguelin including ring truncation have been explored to enhance its pharmacological properties. In this study, the design and straightforward synthesis of a series of B, C, and E (BCE)-ring-truncated deguelin analogues with deoxybenzoin backbone were described. The structure-activity relationships (SARs) were established by evaluation of their inhibitory activities against three cancer cell lines, A549 (adenocarcinomic human alveolar basal epithelial cells), HCT116 (human colorectal cancer cells), and MCF-7 (breast cancer cells). Six derivatives demonstrated significant and selective inhibitory activ

SUBMITTER: Francisco JAP 

PROVIDER: S-EPMC10652367 | biostudies-literature | 2023 Nov

REPOSITORIES: biostudies-literature