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Articles

Topoisomerase I inhibitory and photocleavage activity by ruthenium complexes containing a new polyaza ligand

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Pages 283-290 | Received 25 May 2018, Accepted 24 Aug 2019, Published online: 09 Sep 2019
 

Abstract

Two new ruthenium complexes containing a new polyaza ligand were found to inhibit the DNA supercoiled relaxation mediated by topoisomerase I (topo I), cleave DNA under irradiation and interact with CT-DNA by intercalation. Both complexes exhibited fast singlet oxygen generation rate, and DNA photocleavage reaction should be initiated by 1O2. Furthermore, complex 2 showed higher photocleavage activity, topo I inhibition activity, and DNA affinity than complex 1. This work shows that two complexes can act as DNA binders with high affinity and good DNA photocleavers. Furthermore, complex 2 can act as a good topo I inhibitor.

Additional information

Funding

This work was supported by Natural Science Foundation of Hunan Province (2017JJ2195, 2016JJ6105), China Postdoctoral Science Foundation (2015M582339), Open Project of State Key Laboratory of Chemo/biosensing and Chemometrics (2016010), Research Foundation of Education Bureau of Hunan Province (17B181, 16A145, 15C0935).

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