Synthesis, structure, and biological evaluation of a platinum-carbazole conjugate

Cisplatin resistance is caused, in part, by the efficient removal of the helix‐distorting cisplatin 1,2‐intrastrand cross‐links by nucleotide excision repair ( NER ) machinery. To make a platinum‐ DNA adduct that causes less helical distortion than the cisplatin 1,2‐intrastrand adduct, we designed and synthesized a monofunctional platinum‐carbazole conjugate (carbazoplatin). The 2.5 Å crystal structure of carbazoplatin‐ DNA adduct revealed both...