Carborane-Based Analogues of 5-Lipoxygenase Inhibitors Co-inhibit Heat Shock Protein 90 in HCT116 Cells.,ChemMedChem

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Carborane-Based Analogues of 5-Lipoxygenase Inhibitors Co-inhibit Heat Shock Protein 90 in HCT116 Cells.
ChemMedChem ( IF 3.6 ) Pub Date : 2018-12-21 , DOI: 10.1002/cmdc.201800651
Robert Kuhnert ₁ , Menyhárt-Botond Sárosi ₁ , Sven George ₂ , Peter Lönnecke ₁ , Bettina Hofmann ₂ , Dieter Steinhilber ₂ , Sara Steinmann ₃ , Regine Schneider-Stock ₃ , Blagoje Murganić ₄ , Sanja Mijatović ₄ , Danijela Maksimović-Ivanić ₄ , Evamarie Hey-Hawkins ₁

Affiliation

5-Lipoxygenase converts arachidonic acid into leukotrienes, which are involved in inflammation and angiogenesis. The introduction of carboranes can improve the pharmacokinetic behavior of metabolically less stable pharmaceutics. Herein we report the syntheses of several carborane-based inhibitors of the 5-lipoxygenase pathway. The isosteric replacement of phenyl rings by carboranes leads to improved cytotoxicity toward several melanoma and colon cancer cell lines. For the colon cancer cell line HCT116, the co-inhibition of heat shock protein 90 was observed.

中文翻译：

5-脂氧合酶抑制剂的基于硼烷的类似物共同抑制HCT116细胞中的热激蛋白90。

5-脂氧合酶将花生四烯酸转化为白三烯，与炎症和血管生成有关。碳硼烷的引入可以改善代谢较不稳定的药物的药代动力学行为。在本文中，我们报告了几种基于5脂氧合酶途径的基于硼烷的抑制剂的合成。用碳硼烷等位取代苯环导致对几种黑素瘤和结肠癌细胞系细胞毒性的改善。对于结肠癌细胞系HCT116，观察到热休克蛋白90的共抑制。

更新日期：2018-12-21

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