Photoswitchable Stat3 inhibitors: design, synthesis and anticancer activity study on 2D and 3D breast cancer cell cultures.

ABSTRACT: Stat3 protein is known to be hyperactive in many human cancer cells, including leukaemia, lymphoma, breast, ovarian, lung, and prostate cancer cells. The treatment of most of these cancer types relies on chemotherapy, which encounters various side effects owing to off-target effects of the drugs. Photopharmacology promises to eliminate such off-target effects with the use of photoswitchable drugs. Based on a potent Stat3 inhibitor, in this study, we developed two azobenzene-based photoswitchable inhibitors 2 and 3. Ambient light-exposed compound 2 contained 90% trans isomer, which upon irradiation with a 365 nm light, isomerized to 81% cis isomer, that showed t _1/2 of >38 h at 37 °C. Back-irradiation of the cis-enriched PSS with a 475 nm light yielded

SUBMITTER: Bera S 

PROVIDER: S-EPMC12188466 | biostudies-literature | 2025 Jun

REPOSITORIES: biostudies-literature