Platinum(II) terpyridine complexes with glycosylated acetylide and arylacetylide ligands bind to DNA with binding constants approximately 10(5) mol(-1) dm(3); the glycosylated arylacetylide complexes exhibit emission at lambda(max) approximately 620 nm in water and are up to approximately 100-times higher in potency than the clinical cisplatin drug in killing cancer cells.

A cytotoxic artemisinin derivative conjugated with a fluorescent dansyl moiety was synthesized and its subcellular localization in Hep3B cells was examined. Comparison of the localization signals of the fluorescent artemisinin derivative with organelle specific dyes revealed that endoplasmic reticulum (ER) is the main site of its accumulation.

The synthesis of three fluorophore-appended derivatives of dioscin and polyphyllin D is reported herein. Starting from trillin, dansyl derivatives A-C were prepared in overall yields of 7-12% over 7-10 steps. A study of their behavior in a variety of polar solvents suggests that dansyl derivatives A-C are capable of micellar self-assembly and can maintain cytotoxicities (IC50 = 15-18 muM) against the HeLa carcinoma cell line evaluated by standard MTT assay. [structure: see text]