Premium
Topo I inhibition, DNA photocleavage, Molecular docking and cytotoxicities of two new phenanthroline‐based ruthenium complexes
Author(s) -
Liu XueWen,
Tang YuCai,
Liu NingYi,
Deng YuanQing,
Wang Shan,
Liu Ting,
Chen YuanDao,
Lu JiLin
Publication year - 2020
Publication title -
applied organometallic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.53
H-Index - 71
eISSN - 1099-0739
pISSN - 0268-2605
DOI - 10.1002/aoc.5312
Subject(s) - ruthenium , chemistry , phenanthroline , dna , intercalation (chemistry) , topoisomerase , cytotoxicity , stereochemistry , docking (animal) , imidazole , mtt assay , hydrogen bond , biochemistry , molecule , in vitro , catalysis , crystallography , organic chemistry , medicine , nursing
Two ruthenium complexes containing a new phenanthroline‐based ligand pai (pai = 2‐(5‐(1, 10‐ phenanthroline))‐1H‐acenaphtho[1′,2′:4,5]imidazole) were synthesized and characterized. Two ruthenium complexes were found to cleave DNA under irradiation, interact with CT‐DNA by intercalation. Furthermore, DNA topoisomerase inhibition experiments indicated that complex 2 exhibited higher topoisomerase I inhibition activity (IC 50 = 10 μM) than complex 1 (IC 50 = 40 μM). Molecular modeling studies revealed that complex 2 stabilized Top1cc complex via π‐π interaction and the formation of hydrogen bond. The cytotoxicity of complexes 1 and 2 against Eca‐109 and A549 cells was also evaluate by MTT method, indicating that complex 2 exhibited good anticancer activity against Eca‐109 cells (IC 50 = 17.23 ± 0.22 μM), but two ruthenium complexes displayed weak anticancer activity against A549 cells.