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Three Arene‐Ru(II) compounds of 2‐halogen‐5‐aminopyridine: Synthesis, characterization, and cytotoxicity
Author(s) -
Yan XiaoWei,
Xie YongRong,
Jin ZhiMin,
Hu MaoLin,
Zhou LiangPu
Publication year - 2018
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.3923
Subject(s) - chemistry , ruthenium , titration , 4 aminopyridine , stereochemistry , halogen , crystallography , cytotoxicity , binding constant , fluorescence , absorption (acoustics) , in vitro , medicinal chemistry , nuclear chemistry , binding site , organic chemistry , potassium channel , biochemistry , alkyl , physics , quantum mechanics , acoustics , biology , biophysics , catalysis
Three novel compounds, (η 6 ‐p‐cymene)RuCl 2 (2‐fluoro‐5‐aminopyridine) (compound 1), (η 6 ‐p‐cymene)RuCl 2 (5‐amino‐2‐chlorpyridine) (compound 2) and (η 6 ‐p‐cymene)RuCl 2 (2‐bromo‐ 5‐aminopyridine) (compound 3), were synthesized and characterized. The compound 1 and 3 were determined by X‐ray diffraction, showing a distorted piano‐stool type of geometry with similar bond lengths and angles around the ruthenium. Compound 2 exhibited moderate in vitro activity against A549 and MCF‐7 human cancer cells, the other two lower activities. The UV–vis and fluorescent absorption titrations showed that three compounds binded with CT‐DNA in a minor groove. The intrinsic binding constants (Kb) were calculated to be 2.13(±0.03) × 10 5 M −1 , 2.89(±0.03) × 10 5 M −1 and 2.45(±0.03) × 10 5 M −1 for compound 1, 2 and 3, respectively, by using UV–vis absorption titrations data. Among the three compound, the highest value of intrinsic binding constant of compound 2 was consistent with its highest cytoxicity against A549 and MCF‐7 human cancer cells in vitro .