Thirteen new ruthenium amino acid complexes were synthesized and characterized. They were obtained by the reaction of α-amino acids (AA) with [RuCl₂(P-P)(N-N)], where P-P = 1,4-bis(diphenylphosphino)butane (dppb) or 1,3-bis(diphenylphosphino)propane (dppp) and N-N = 4,4′-dimethyl-2,2′-bipyridine (4′-Mebipy), 5,5′-dimethyl-2,2′-bipyridine (5′-Mebipy) or 4,4′-Methoxy-2-2′-bipyridine (4′-MeObipy). This afforded a family of complexes formulated as [Ru(AA-H)(P-P)(N-N)]PF₆, where AA = glycine (Gly), L-alanine (Ala), L-valine (Val), L-tyrosine (Tyr), L-tryptophan (Trp), L-histidine (His) and L-methionine (Met). All compounds were characterized by elemental analysis, spectroscopic and electrochemical techniques. The [Ru(AA-H)(P-P)(N-N)]PF₆ complexes are octahedral (the AA-H ligand binding involves N-amine and O-carboxylate), diamagnetic (low-spin d⁶, S = 0) and present bands due to electronic transitions in the visible region. ¹H, ¹³C{¹H} and ³¹P{¹H} NMR spectra of the complexes indicate the presence of C₂ symmetry, and the identification of diastereoisomers. In vitro cytotoxicity assays of the compounds and cisplatin were carried out using MDA-MB-231 (human breast) tumor cell line and a non-tumor breast cell line (MCF-10A). Most complexes present promising results with IC₅₀ values comparable with the reference drug cisplatin and high selectivity indexes were found for the complexes containing L-Trp. The binding of two Ru-precursors of the type [RuCl₂(dppb)(NN)] (N-N = 4′-MeObipy or 4′-Mebipy) to the blood transporter protein human serum albumin (HSA) was evaluated by fluorescence and circular dichroism spectroscopy. Both complexes bind HSA, probably in the hydrophobic pocket near Trp214, and the Ru-complex containing 4′-MeObipy shows higher affinity for HSA than the 4′-Mebipy one.

合成并表征了十三种新的钌氨基酸复合物。它们是通过α-氨基酸（AA）与[RuCl ₂（PP）（NN）]反应得到的，其中PP = 1,4-双（二苯基膦基）丁烷（dppb）或1,3-双（二苯基膦基）丙烷（dppp）和NN = 4,4'-二甲基-2,2'-联吡啶（4'-Mebipy），5,5'-二甲基-2,2'-联吡啶（5'-Mebipy）或4,4 ′-甲氧基-2-2′-联吡啶（4′-MeObipy）。这提供了一系列配制成[Ru（AA-H）（PP）（NN）] PF ₆的配合物，其中AA =甘氨酸（Gly），L-丙氨酸（Ala），L-缬氨酸（Val），L-酪氨酸（Tyr），L-色氨酸（Trp），L-组氨酸（His）和L-蛋氨酸（Met）。所有化合物均通过元素分析，光谱学和电化学技术进行了表征。[Ru（AA-H）（PP）（NN）] PF ₆络合物为八面体（AA-H配体结合涉及N-胺和O-羧酸盐），抗磁性（低旋d ⁶，S  =  0），并且由于可见区中的电子跃迁而出现能带。^{配合物的1} H，¹³ C { ¹ H}和³¹ P { ¹ H} NMR光谱表明存在C ₂对称性，并且鉴定了非对映异构体。使用MDA-MB-231（人乳腺）肿瘤细胞系和非肿瘤乳腺细胞系（MCF-10A）进行化合物和顺铂的体外细胞毒性测定。大多数配合物使用IC _50均显示出令人鼓舞的结果对于含有L-Trp的复合物，发现其值可与参比药物顺铂相当，并且具有较高的选择性指数。通过荧光和荧光法评估了两种[RuCl ₂（dppb）（N N）]型Ru前体（NN = 4'-MeObipy或4'-Mebipy）与血液转运蛋白人血清白蛋白（HSA）的结合。圆二色谱。两种复合物都可能在Trp214附近的疏水口袋中结合HSA，并且含有4'-MeObipy的Ru复合物对HSA的亲和力高于4'-Mebipy。