A Family of Rhodium Complexes with Selective Toxicity toward Mismatch Repair-Deficient Cancers.

ABSTRACT: Rhodium metalloinsertors are a unique set of metal complexes that bind specifically to DNA base pair mismatches in vitro and kill mismatch repair (MMR)-deficient cells at lower concentrations than their MMR-proficient counterparts. A family of metalloinsertors containing rhodium-oxygen ligand coordination, termed "Rh-O" metalloinsertors, has been prepared and shown to have a significant increase in both overall potency and selectivity toward MMR-deficient cells regardless of structural changes in the ancillary ligands. Here we describe DNA-binding and cellular studies with the second generation of Rh-O metalloinsertors in which an ancillary ligand is varied in both steric bulk and lipophilicity. These complexes, of the form [Rh(L)(chrysi)(PPO)]²⁺, all include the O-containing PP

SUBMITTER: Boyle KM 

PROVIDER: S-EPMC5965675 | biostudies-literature | 2018 Apr

REPOSITORIES: biostudies-literature