Anticancer metallohelices: nanomolar potency and high selectivity.

ABSTRACT: A range of new helicate-like architectures have been prepared via highly diastereoselective self-assembly using readily accessible starting materials. Six pairs of enantiomers [Fe₂L₃]Cl₄·nH₂O (L = various bidentate ditopic ligands NN-NN) show very good water solubility and stability. Their activity against a range of cancer cell lines in vitro is structure-dependent and gives IC₅₀ values as low as 40 nM. In an isogenic pair of HCT116 colorectal cancer cells, preferential activity was observed against cell lines that lack functional p53. Selectivity is also excellent, and against healthy human retinal pigment epithelial (ARPE19) and lung fibroblast (WI38) cells IC₅₀ values are nearly three orders of magni

SUBMITTER: Kaner RA 

PROVIDER: S-EPMC5530816 | biostudies-literature | 2016 Feb

REPOSITORIES: biostudies-literature