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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Synthesis, characterisation and biological evaluation of N-(ferrocenyl)naphthoyl amino acid esters as anticancer agents
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Synthesis, characterisation and biological evaluation of N-(ferrocenyl)naphthoyl amino acid esters as anticancer agents

机译：N-（二茂铁基）萘甲酰基氨基酸酯类抗癌药的合成，表征及生物学评价

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摘要

A series of N-(ferrocenyl)naphthoyl amino acid esters 5-18 has been prepared by coupling ferrocenyl naphthoic acids 3-4 to α-amino acids and linear amino acids in the presence of N-(3-dimethylaminopropyl)-N′- ethylcarbodiimide hydrochloride (EDC) and 1-hydroxybenzotriazole (HOBt). The compounds were fully characterised by a range of NMR spectroscopic techniques, UV-Vis spectroscopy, mass spectrometry and cyclic voltammetry. X-ray crystallographic studies of the intermediate compounds 1-2 were also performed. Biological evaluation of the intermediates 1-2 and N-(ferrocenyl)naphthoyl amino acid esters 5-18 was performed in the H1299 non-small cell lung cancer (NSCLC) cell line and the Sk-Mel-28 metastatic melanoma cell line. The intermediates 1-2 failed to produce an effect in either cell line. Compounds 5-18 exhibited a strong anti-proliferative effect in the H1299 cell line, whilst the Sk-Mel-28 cells were slightly more resistant to these compounds. N-(6-ferrocenyl-2- naphthoyl)-γ-aminobutyric acid ethyl ester 17 shows a particularly high activity in both the H1299 cell line (IC_(50) = 0.62 ± 0.07 μM) and the Sk-Mel-28 cell line (IC_(50) = 1.41 ± 0.04 μM).
机译：在N-（3-二甲基氨基丙基）-N'-存在下，通过将二茂铁基萘甲酸3-4与α-氨基酸和线性氨基酸偶联，制备了一系列N-（二茂铁基）萘基氨基酸酯5-18。乙基碳二亚胺盐酸盐（EDC）和1-羟基苯并三唑（HOBt）。通过一系列NMR光谱技术，UV-Vis光谱，质谱和循环伏安法对化合物进行了全面表征。还进行了中间体化合物1-2的X射线晶体学研究。在H1299非小细胞肺癌（NSCLC）细胞系和Sk-Mel-28转移性黑色素瘤细胞系中进行了中间体1-2和N-（二茂铁基）萘甲酰基氨基酸酯5-18的生物学评估。中间体1-2在任一细胞系中均未产生作用。化合物5-18在H1299细胞系中表现出强大的抗增殖作用，而Sk-Mel-28细胞则对这些化合物具有更高的抗性。 N-（6-二茂铁基-2-萘甲酰基）-γ-氨基丁酸乙酯17在H1299细胞系（IC_（50）= 0.62±0.07μM）和Sk-Mel-28细胞系中均显示特别高的活性（IC_（50）= 1.41±0.04μM）。

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