biostudies-literatureYu FCReserve Talent Foundation of Yunnan Province for Middle-aged and Young Academic and Technical LeadersMinistry of Education of the People's Republic of ChinaNational Natural Science Foundation of China873-889https://www.ebi.ac.uk/biostudies/studies/S-EPMC6044579biostudies-literatureUnknown2(3)Self-labeled inhibitors (SLIs) are promising for creating links, ranging from cancer therapy and metastatic pathways to mechanistic elucidation. In this study, a new category of "two-in-one" fluorescent xanthone inhibitors was developed for the systematic evaluation of anticancer activity and the selective imaging of cytoplasm in vitro. These xanthone inhibitors presented high fluorescent brightness, working over a wide pH range enabled by a "switchable reaction" of the heterocyclic backbone. The strength and nature of fluorescence were probed via spectroscopic methods and density functional theory calculations on the molecular level, respectively. Along with the potent anticancer activity, which was demonstrated using MTT and clonogenic assays with high fluorescent brightness in the cytopACS omegaBeyond the Antagonism: Self-Labeled Xanthone Inhibitors as Modeled "Two-in-One" Drugs in Cancer Therapy.PMC604457921262042812605012012HB001IRT1309521662042U120222121362042Lin XRLiu FFMa YLZhang JHQu WWYan SJYu FCLin JLiu ZCWu WfalseBeyond the Antagonism: Self-Labeled Xanthone Inhibitors as Modeled "Two-in-One" Drugs in Cancer Therapy.Self-labeled inhibitors (SLIs) are promising for creating links, ranging from cancer therapy and metastatic pathways to mechanistic elucidation. In this study, a new category of "two-in-one" fluorescent xanthone inhibitors was developed for the systematic evaluation of anticancer activity and the selective imaging of cytoplasm in vitro. These xanthone inhibitors presented high fluorescent brightness, working over a wide pH range enabled by a "switchable reaction" of the heterocyclic backbone. The strength and nature of fluorescence were probed via spectroscopic methods and density functional theory calculations on the molecular level, respectively. Along with the potent anticancer activity, which was demonstrated using MTT and clonogenic assays with high fluorescent brightness in the cytop2017-01-01T00:00:00Z2017 Mar2026-05-05T23:41:58.839Z2025-05-29T20:27:32.298ZS-EPMC60445793002361710.1021/acsomega.6b00545