Front Cover: Hybrid Androgen Receptor Inhibitors Outperform Enzalutamide and EPI‐001 in in vitro Models of Prostate Cancer Drug Resistance (ChemMedChem 2/2023)

Abstract

The Front Cover shows the design of the dual inhibitors starting from the FDA-approved enzalutamide (pink) and EPI-001 (green). On the right, in grey, we have the androgen receptor protein. Herein we present the schematic design of the most potent analogue in killing in vitro models of prostate cancer drug resistance, which was designed by covalently linking the two drugs using a PEG triazole linker (in cyan). The paper describes the synthesis of the compounds and their full biological characterisation. More information can be found in the Research Article by Radu Costin Bizga Nicolescu, Zoe R. Maylin Mohammad Asim, David R. Spring et al.