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New Silver Complexes with Mixed Thiazolidine and Phosphine Ligands as Highly Potent Antimalarial and Anticancer Agents

机译:新型混合噻唑烷和膦配体的银配合物作为高效抗疟和抗癌剂

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Five silver(I) complexes containing a mixed ligand system of phosphine and thiazolidine were successfully synthesized. The structural information of the complexes was assembled using various spectroscopic techniques such as CHN elemental analysis, Fourier transformed infrared (FTIR), 1H, 13C, and 31P{1H} NMR spectroscopy, and thermogravimetric analysis (TGA). A bidentate phosphine ligand acted as a chelating agent which bond to the silver in 1  2 molar ratios. Meanwhile, thiazolidine was attached to the silver in a 1  1 molar ratio. The antiplasmodial properties of all synthesized complexes were investigated on chloroquine-resistant P. falciparum parasite via HRP2 assays and cytotoxicity tests on Vero cells. Of all the synthesized complexes, complex 2 showed the highest SI value (more than 12.4) followed by complex 5 (6.6). The potent properties of compounds 2 and 5 were also noted in the in vitro antiproliferative assays involving MDA-MB-231 and MCF-7 breast cancer cell lines as well as HT-29 colon cancer cell line. Complex 2 was selective for MDA-MB-231 cells (GI50 = 1.9 ± 0.3 µM), while complex 5 acted predominantly on breast carcinoma cells (GI50 MDA-MB-231 = 4.7 ± 1.1 µM; MCF-7 = 2.9 ± 0.9 µM) instead of colon carcinoma (HT-29) cells (GI50 = 15.1 ± 1.9 µM).
机译:成功合成了五种包含膦和噻唑烷混合配体系统的银(I)配合物。使用各种光谱技术(例如CHN元素分析,傅立叶变换红外(FTIR),1H,13C和31P {1H} NMR光谱和热重分析(TGA))来组装复合物的结构信息。二齿膦配体充当螯合剂,以1 2摩尔比与银键合。同时,噻唑烷以1∶1的摩尔比附着在银上。通过HRP2分析和对Vero细胞的细胞毒性测试,研究了所有合成配合物在抗氯喹恶性疟原虫上的抗血浆特性。在所有合成的配合物中,配合物2的SI值最高(大于12.4),其次是配合物5的6.6。在涉及MDA-MB-231和MCF-7乳腺癌细胞系以及HT-29结肠癌细胞系的体外抗增殖试验中,也注意到了化合物2和5的有效特性。复合物2对MDA-MB-231细胞具有选择性(GI50 = 1.9±0.3μM),而复合物5主要作用于乳腺癌细胞(GI50 MDA-MB-231 = 4.7±1.1μM; MCF-7 = 2.9±0.9μM )代替结肠癌细胞(HT-29)(GI50 = 15.1±1.9 µM)。

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