奈特在元素周期表中的移动,从铜到铂,新型抗肿瘤混合螯合铜化合物,Casiopeinas,通过体外人和小鼠癌细胞系小组评估。

I Gracia-Mora, L Ruiz-Ramírez, C Gómez-Ruiz, M Tinoco-Méndez, A Márquez-Quiñones, L R Lira, A Marín-Hernández, L Macías-Rosales, M E Bravo-Gómez
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引用次数: 69

摘要

我们合成了一种基于混合螯合铜(II)配合物的新型抗癌剂,命名为Casiopeínas(R),其通式为[Cu(N-N)(N-O)H(2)O]NO(3)(其中,N-N =二亚胺为1,10-菲罗啉,2,2-联吡啶,或取代,N-O=氨基醋酯或[Cu(N-N)(O-O)H(2)O]NO(3))(其中NN=二亚胺为10-菲罗啉,2,2-联吡啶或取代Casiopeínas I, II, IV, V, VI, VII VIII和O-O=乙酰丙酮,我们使用人类癌细胞组和一些尿癌细胞来评估其体外抗肿瘤活性。对11种Casiopeinas进行了评价,以获得一些结构-活性相关性和一些单齿Casiopeinäs类似物;顺铂作为对照药物。在所有情况下,Casiopeina的浓度比顺铂低10或100倍,观察到50%的生长抑制。在以前的工作中,我们报道了Casiopeina II诱导细胞凋亡。结果表明,Casiopeinass是一种有前景的新型抗癌候选药物,值得进一步开发用于临床试验。
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Knigth's Move in the Periodic Table, From Copper to Platinum, Novel Antitumor Mixed Chelate Copper Compounds, Casiopeinas, Evaluated by an in Vitro Human and Murine Cancer Cell Line Panel.

We synthesized a novel anticancer agents based on mixed chelate copper (II) complexes, named Casiopeínas((R)) has of general formula [Cu(N-N)(N-O)H(2)O]NO(3) (where, N-N = diimines as 1,10- phenanthroline, 2,2-bipyridine, or substituted and N-O=aminoeidate or [Cu(N-N)(O-O)H(2)O]NO(3) (where NN= diimines as 10-phenanthroline, 2,2-bipyridine or substituted Casiopeínas I, II, IV, V, VI, VII VIII and O-O=acetylacetonate, salicylaldehidate Casiopínas III). We evaluated the in vitro antitumor activity using a human cancer cell panel and some nurine cancer cells. Eleven Casiopeinas are evaluated in order to acquire some structure-activity correlations and some monodentated Casiopeinäs analogues; cisplatinum was used as control drug. The 50% growth inhibition observed is, in all cases reach with concentrations of Casiopeina's 10 or 100 times lower than cisplatinum. In a previous work we reported the induction of apoptosis by Casiopeina II. The results indicate that Casiopeinass are a promising new anticancer drug candidates to be developed further toward clinical trials.

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