Quinoline-Conjugated Ruthenacarboranes: Toward Hybrid Drugs with a Dual Mode of Action.,ChemMedChem

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Quinoline-Conjugated Ruthenacarboranes: Toward Hybrid Drugs with a Dual Mode of Action.
ChemMedChem ( IF 3.6 ) Pub Date : 2019-11-19 , DOI: 10.1002/cmdc.201900349
Marta Gozzi ₁ , Blagoje Murganic ₂ , Dijana Drača ₂ , John Popp ₁ , Peter Coburger ₁ , Danijela Maksimović-Ivanić ₂ , Sanja Mijatović ₂ , Evamarie Hey-Hawkins ₁

Affiliation

The role of autophagy in cancer is often complex, ranging from tumor-promoting to -suppressing effects. In this study, two novel hybrid molecules were designed, containing a ruthenacarborane fragment conjugated with a known modulator of autophagy, namely a quinoline derivative. The complex closo-[3-(η6 -p-cymene)-1-(quinolin-8-yl-acetate)-3,1,2-RuC2 B9 H10 ] (4) showed a dual mode of action against the LN229 (human glioblastoma) cell line, where it inhibited tumor-promoting autophagy, and strongly inhibited cell proliferation, de facto blocking cellular division. These results, together with the tendency to spontaneously form nanoparticles in aqueous solution, make complex 4 a very promising drug candidate for further studies in vivo, for the treatment of autophagy-prone glioblastomas.

中文翻译：

喹啉共轭钌碳硼烷：具有双重作用模式的混合药物。

自噬在癌症中的作用通常很复杂，从促进肿瘤到抑制肿瘤。在这项研究中，设计了两种新型杂化分子，其中含有与已知的自噬调节剂（即喹啉衍生物）缀合的钌碳硼烷片段。复合物 closo-[3-(η6 -p-cymene)-1-(quinolin-8-yl-acetate)-3,1,2-RuC2 B9 H10 ] (4) 显示出针对 LN229 的双重作用模式（人胶质母细胞瘤）细胞系，它抑制肿瘤促进自噬，并强烈抑制细胞增殖，事实上阻止细胞分裂。这些结果，加上在水溶液中自发形成纳米颗粒的倾向，使得复合物 4 成为一种非常有前途的候选药物，可用于进一步的体内研究，用于治疗易发生自噬的胶质母细胞瘤。

更新日期：2019-11-20

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