State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Pharmacy, Guangxi Normal University, 15 Yucai Road, Guilin 541004, PR China.
State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Pharmacy, Guangxi Normal University, 15 Yucai Road, Guilin 541004, PR China; Guangxi Key Lab of Agricultural Resources Chemistry and Biotechnology, College of Chemistry and Food Science, Yulin Normal University, 1303 Jiaoyudong Road, Yulin 537000, PR China.
J Inorg Biochem. 2018 Dec;189:143-150. doi: 10.1016/j.jinorgbio.2018.09.004. Epub 2018 Sep 24.
Eight new platinum(II) complexes Pt1-Pt8 with substituted 3‑(2'‑benzimidazolyl) coumarins were successfully synthesized and characterized by single crystal X-ray diffraction analysis, nuclear magnetic resonance spectroscopy (NMR), electrospray ionization-mass spectrometry (ESI-MS), infrared spectrophotometry (IR) and elemental analysis. Crystallographic data of these Pt1-Pt8 complexes showed that the Pt(II) has distorted four-coordinated square planar geometry. Pt1-Pt8 were found to display high cytotoxic activity in vitro against the cisplatin-resistant SK-OV-3/DDP cancer cells with a low IC from 1.01-10.32 μM, but low cytotoxicity on the normal HL-7702 cells. Further studies revealed that Pt1-Pt3 induced apoptosis in SK-OV-3/DDP cancer cells via mitochondria dysfunction signaling pathways. Our findings also indicated that Pt1 was a telomerase inhibitor targeting c-myc promoter elements.
八个新型的含取代 3-（2'-苯并咪唑基）香豆素的铂（II）配合物 Pt1-Pt8 通过单晶 X 射线衍射分析、核磁共振波谱（NMR）、电喷雾电离质谱（ESI-MS）、红外光谱（IR）和元素分析成功合成并进行了表征。这些 Pt1-Pt8 配合物的晶体学数据表明，Pt(II) 具有扭曲的四配位平面四方几何结构。Pt1-Pt8 被发现对顺铂耐药的 SK-OV-3/DDP 癌细胞具有高体外细胞毒性活性，IC 从 1.01-10.32 μM 不等，而对正常 HL-7702 细胞的细胞毒性较低。进一步的研究表明，Pt1-Pt3 通过线粒体功能障碍信号通路诱导 SK-OV-3/DDP 癌细胞凋亡。我们的研究结果还表明，Pt1 是一种针对 c-myc 启动子元件的端粒酶抑制剂。
