Organometallic Glutathione S-Transferase Inhibitors,Organometallics

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Organometallic Glutathione S-Transferase Inhibitors
Organometallics ( IF 2.5 ) Pub Date : 2017-08-24 00:00:00 , DOI: 10.1021/acs.organomet.7b00468
Emilia Păunescu ₁ , Mylène Soudani ₁ , Paloma Martin ₂ , Rosario Scopelliti ₁ , Mario Lo Bello ₂ , Paul J. Dyson ₁

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A new family of organometallic p-cymene ruthenium(II) and osmium(II) complexes conjugated to ethacrynic acid, a glutathione transferase (GST) inhibitor, is reported. The ethacrynic acid moiety (either one or two) is tethered to the arene ruthenium(II) and osmium(II) fragments via strongly coordinating modified bipyridine ligands. The solid-state structure of one of the complexes, i.e. [Os(η⁶-p-cymene)Cl][(4′-methyl-[2,2′-bipyridin]-4-yl)methyl-2-(2,3-dichloro-4-(2-methylenebutanoyl)phenoxy)acetate]Cl, was established by single-crystal X-ray diffraction, corroborating the expected structure. The complexes are efficient inhibitors of GST P1-1, an enzyme expressed in cancer cells and implicated in drug resistance, and are cytotoxic to the GST-overexpressing chemoresistant A2780cisR ovarian cancer cell line.

中文翻译：

有机金属谷胱甘肽S-转移酶抑制剂

谷胱甘肽转移酶（GST）抑制剂，新的有机金属对-Cymene钌（II）和（II）配合物与乙炔酸共轭的报道。乙炔酸部分（一个或两个）通过强配位的联吡啶配体与芳烃钌（II）和（II）片段相连。的配合物，即[Os中的一项所述的固态结构（η ⁶ - p-柠檬烯）Cl] [（4'-甲基-[2,2'-联吡啶] -4-基）甲基-2-（2,3-二氯-4-（2-亚甲基丁酰基）苯氧基）乙酸] Cl是通过单晶X射线衍射确定，证实了预期的结构。该复合物是GST P1-1的有效抑制剂，GST P1-1是一种在癌细胞中表达并与耐药有关的酶，并且对过表达GST的化学抗性A2780cisR卵巢癌细胞系具有细胞毒性。

更新日期：2017-08-25

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