Pd (II)‐PPh 3 complexes of halogen substituted acylthiourea ligands: Biomolecular interactions and in vitro anti‐proliferative activity
Pd (II)‐PPh
3
complexes of halogen substituted acylthiourea ligands: Biomolecular interactions and
in vitro
anti‐proliferative activity
复制标题
卤素取代的酰基硫脲配体的 Pd (II)-PPh 3 配合物：生物分子相互作用和体外抗增殖活性
DOI：
10.1002/aoc.6765
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发表时间：
2022
影响因子：
3.9
通讯作者：
R. Karvembu
中科院分区：
文献类型：
--
作者：
D. P. Dorairaj;J. Haribabu;Yu‐Lun Chang;C. Echeverria;S. C. Hsu;R. Karvembu
本文报道了四种新的酰基硫脲钯配合物（C1-C4）的合成，并研究了卤素取代的酰基硫脲配体对其配合物生物应用的影响。通过各种光谱和分析方法对配合物进行了表征。通过单晶X射线衍射研究证实了配合物的扭曲正方形平面几何形状，这也揭示了配体与Pd（II）的双齿（N，S）配位。通过光谱和对接工具研究了配合物与生物分子（DNA/BSA）的相互作用。所有配合物均表现出与靶向生物分子良好的结合能力。此外，通过对癌症（HeLa-宫颈、HCT 116-结肠直肠和HepG 2-肝）和正常（HEK 293-胚胎肾）细胞系进行MTT测定来研究复合物的体外抗增殖活性。所有配合物对三种癌细胞均有明显的抑制作用，其中含氯取代酰基硫脲的配合物C2对HeLa细胞的抑制作用上级强，其IC_（50）值为6.5 μM，高于顺铂。采用AO/EB、DAPI、DNA梯状电泳和流式细胞术检测C2诱导HeLa细胞凋亡。最后，通过细胞周期分析检测了C2的凋亡效率，其中复合物诱导HeLa细胞的细胞周期停滞在G 0/G1期。
Herein, we report the synthesis of four new Pd(II) acylthiourea complexes (C1–C4) to study the effect of halogen substituted acylthiourea ligands on the biological applications of their Pd(II)–PPh3complexes. The complexes were characterized by various spectroscopic and analytical methods. The distorted square planar geometry of complexes was confirmed by single crystal X‐ray diffraction study, which also revealed the bidentate (N, S) coordination of the ligands with Pd(II). Interactions of the complexes with biomolecules (DNA/BSA) were investigated by spectroscopic and docking tools. All the complexes showed good binding ability with the targeted biomolecules. Further,in vitroanti‐proliferative activity of the complexes was investigated by performing MTT assay on cancer (HeLa‐cervical, HCT116‐colorectal, and HepG2‐hepatic) and normal (HEK293‐embryonic kidney) cell lines. All the complexes displayed remarkable activity on the three cancer cells, and among them, complexC2bearing chlorine substituted acylthiourea showed superior activity on HeLa cells with an IC50value of 6.5 μM, which was higher than that of cisplatin. Apoptosis induced byC2on HeLa cells was assessed by AO/EB, DAPI and DNA laddering assays, and flow cytometry. Finally, the apoptotic efficiency ofC2was tested by cell cycle analysis, wherein the complex induced the cell cycle arrest in HeLa cells at G0/G1 phase.