Fig. 2
From: Ligands stimulating antitumour immunity as the next G-quadruplex challenge
Cytotoxicity potency of anticancer DNA-interacting agents. Violin plots showing IC50 values of selected DNA-interacting agents with established anticancer activity in standard chemotherapy of human tumours. Data were obtained from “Genomics of Drug Sensitivity in Cancer” (GDSC) database [40], which includes information from around one thousands cancer cell lines (www.cancerrxgene.org). Drugs are classified on the base of their mechanism of action and ranked by cytotoxicity (left to right). G4 stabilizers have a lower cytotoxic potency than topoisomerase poisons, microtubule interactors, Mitomycin C and Dactinomycin (Actinomycin D). Alkylating agents and cross-linkers can react with cytoplasmic nucleophilic groups in cells, effectively lowering their nuclear concentrations [41]. Moreover, PARP inhibitors are mainly used in BRCAness tumours where their cell killing potency is much increased due to mutations or deletion of BRCA genes [42]. Therefore, G4 binders (Pyridostatin and CX-5461) have a low cytotoxic potency in comparison to other effective DNA-interacting anticancer agents