Topoisomerases (TOPO) are DNA enzymes that play an essential role in many cellular processes like DNA replication, transcription, chromosome condensation, and, most importantly, in the mitosis to decatenate the daughter chromosomes. Topoisomerase is the targeted enzyme for cancer chemotherapy as they control the topology of DNA. There were several nonmetallic synthetic topoisomerase inhibitors proposed in recent years. Few metal complexes are also known as dual topoisomerase inhibitors. Total six copper complexes of 2-hydroxy-(3R)-1,4-naphthoquinone-1-oxime (R = H (1) in Cu-1 and Cu-2, -CH3 (2) in Cu-3 and Cu-4 and –Cl (3) in Cu-5 and Cu-6) targeted as topoisomerase II inhibitors. Naphthoquinoneoxime ligands are noninnocent and coordinate with metal ions as monoanionic or dianionic forms. These ligands also exist in the keto-enol tautomeric form in polar solvents. Tautomeric forms can be separated and isolated by HPLC. Complexes Cu-1, Cu-3, and Cu-5 are complexes of ligands 1, 2, and 3, respectively, while complexes Cu-2, Cu-4, and Cu-6 contain either pyridine as a cation or present in lattice. Cu-2; [Cu(1)2]py+ crystallizes in monoclinic P21/c space group, one of the naphthoquinoneoxime ligand coordinates to Cu2+ ion in dianionic form. Copper-Copper distance is 3.22 Å in the stacked dimer. A tetrameric complex Cu-4 crystallizes in triclinic P-1 space group, the ligand 2-hydroxy-3-methyl-1,4-naphthoquinone-1-oxime coordinate to Cu2+ ion in keto as well as enol form adjudged by carbonyl distances from single-crystal X-ray structure. Topoisomerase II inhibition, DNA Cleavage assay, and growth inhibition assay were performed on all six copper complexes along with their parent ligands as well as the precursor copper salts.

Copper–naphthoquinoneoxime complexes as topoisomerase inhibitors: Crystallography evidence for keto-enol coordination of 2-hydroxy-3-methyl-1,4-naphthoquinone-1-oxime

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ACS Spring 2020 National Meeting & Expo

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