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Synthesis, characterization and biological evaluation of Pd(ii), Cu(ii), Re(i) and 99mTc(i) thiazole-based complexes†
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2018-04-13 00:00:00 , DOI: 10.1039/c8md00067k Jelena M Mašković 1 , Antonios Hatzidimitriou 2 , Ana Damjanović 3 , Tatjana P Stanojković 3 , Srećko R Trifunović 4 , Athina A Geronikaki 5 , Dionysia Papagiannopoulou 5
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2018-04-13 00:00:00 , DOI: 10.1039/c8md00067k Jelena M Mašković 1 , Antonios Hatzidimitriou 2 , Ana Damjanović 3 , Tatjana P Stanojković 3 , Srećko R Trifunović 4 , Athina A Geronikaki 5 , Dionysia Papagiannopoulou 5
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A new thiazole-containing multidentate ligand 2-((2-phenylthiazol-4-yl)methylthio)ethanamine, L, was synthesized and used to prepare new complexes of the formula PdIILCl2 (Pd–L), CuIIL2Cl2 (Cu–L) and fac-[Re/99mTcI(CO)3(L)]+ (Re/99mTc–L). The ligand L and the metal complexes were characterized spectroscopically. Furthermore, the structures of Re–L and Cu–L were elucidated by X-ray crystallography. Ligand L acts as a bidentate (Nth, S) chelator in Pd–L, as a bidentate (N, S) chelator in Cu–L and as a tridentate (Nth, S, N) chelator in Re–L. The radiotracer 99mTc–L was synthesized in high yield and characterised by HPLC comparison with the Re–L analog. The synthesized compounds were evaluated for their anti-inflammatory and cytotoxic properties. The compounds exhibited low anti-inflammatory activity with Pd–L showing the highest activity among them. The cytotoxic activity of the ligand and the complexes against several human cancer cell lines (cervical adenocarcinoma HeLa, colorectal adenocarcinoma LS-174T, lung adenocarcinoma A549, breast adenocarcinoma MDA-MB-231 and normal human lung fibroblast cell line MRC-5) was examined using the MTT assay. The complex Cu–L exhibited the highest cytotoxicity and the complex Pd–L showed the best tumor selectivity. The changes in the cell cycle phase distribution were determined by flow cytometry and it was found that ligand L shows the highest apoptotic activity. The biodistribution studies of 99mTc–L in mice showed fast tissue clearance. Of all the thiazole-containing compounds, the palladium complex appears to be more promising for future efforts.
中文翻译：
Pd(ii)、Cu(ii)、Re(i) 和 99mTc(i) 噻唑基配合物的合成、表征和生物学评价†
合成了一种新的含噻唑多齿配体 2-((2-苯基噻唑-4-基)甲硫基)乙胺 L，并用于制备新的复合物，分子式为 Pd II LCl 2 (Pd-L) Cu II L 2 Cl 2 (Cu–L) 和fac -[Re/ 99m Tc I (CO) 3 (L)] + (Re/ 99m Tc–L)。配体 L 和金属配合物通过光谱进行表征。此外，通过 X 射线晶体学阐明了 Re-L 和 Cu-L 的结构。配体 L 在 Pd-L 中充当二齿 (N th , S) 螯合剂，在 Cu-L 中充当二齿 (N, S) 螯合剂和三齿 (N th, S, N) Re-L 中的螯合剂。放射性示踪剂99mTc-L 以高产率合成，并通过 HPLC 与 Re-L 类似物的比较来表征。评估了合成的化合物的抗炎和细胞毒性特性。这些化合物表现出低抗炎活性，其中 Pd-L 表现出最高的活性。检测了配体和复合物对几种人类癌细胞系（宫颈腺癌 HeLa、结肠直肠癌 LS-174T、肺腺癌 A549、乳腺癌 MDA-MB-231 和正常人肺成纤维细胞系 MRC-5）的细胞毒活性使用 MTT 法。复合物Cu-L表现出最高的细胞毒性，复合物Pd-L表现出最好的肿瘤选择性。通过流式细胞仪测定细胞周期时相分布的变化，发现配体L显示出最高的凋亡活性。小鼠中的99m Tc-L 显示出快速的组织清除。在所有含噻唑化合物中，钯络合物似乎更有希望用于未来的研究。
更新日期：2018-04-13
中文翻译：
Pd(ii)、Cu(ii)、Re(i) 和 99mTc(i) 噻唑基配合物的合成、表征和生物学评价†
合成了一种新的含噻唑多齿配体 2-((2-苯基噻唑-4-基)甲硫基)乙胺 L，并用于制备新的复合物，分子式为 Pd II LCl 2 (Pd-L) Cu II L 2 Cl 2 (Cu–L) 和fac -[Re/ 99m Tc I (CO) 3 (L)] + (Re/ 99m Tc–L)。配体 L 和金属配合物通过光谱进行表征。此外，通过 X 射线晶体学阐明了 Re-L 和 Cu-L 的结构。配体 L 在 Pd-L 中充当二齿 (N th , S) 螯合剂，在 Cu-L 中充当二齿 (N, S) 螯合剂和三齿 (N th, S, N) Re-L 中的螯合剂。放射性示踪剂99mTc-L 以高产率合成，并通过 HPLC 与 Re-L 类似物的比较来表征。评估了合成的化合物的抗炎和细胞毒性特性。这些化合物表现出低抗炎活性，其中 Pd-L 表现出最高的活性。检测了配体和复合物对几种人类癌细胞系（宫颈腺癌 HeLa、结肠直肠癌 LS-174T、肺腺癌 A549、乳腺癌 MDA-MB-231 和正常人肺成纤维细胞系 MRC-5）的细胞毒活性使用 MTT 法。复合物Cu-L表现出最高的细胞毒性，复合物Pd-L表现出最好的肿瘤选择性。通过流式细胞仪测定细胞周期时相分布的变化，发现配体L显示出最高的凋亡活性。小鼠中的99m Tc-L 显示出快速的组织清除。在所有含噻唑化合物中，钯络合物似乎更有希望用于未来的研究。
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