Discovery and Evaluation of Novel Sulfonamide Derivatives Targeting Aromatase in ER+ Breast Cancer.

ABSTRACT: Background: Third-generation aromatase inhibitors (CYP19A1) are the mainstay of treatment for estrogen-receptor-positive breast cancer. This is because estrogen is required for cancer growth in approximately 70% of patients with this condition. Although potent and effective, aromatase inhibitors induce resistance and secondary effects, requiring treatment to be discontinued. This clinical limitation highlights the need to search for new molecules. Previous studies have led to the identification of a set of indole sulfonamide molecules that exhibit interesting activity against aromatase. Methods: Phenyl and benzyl sulfonamide derivatives with alkylated heterocycles linked by short methylene bridges were designed and synthesized. The aromatase inhibition and cytotoxicity were t

SUBMITTER: De Filippis B 

PROVIDER: S-EPMC12389619 | biostudies-literature | 2025 Aug

REPOSITORIES: biostudies-literature