Carborane-based analogues of 5-lipoxygenase inhibitors co-inhibit heat shock protein 90 in HCT-116 cells.

Carborane-based analogues of 5-lipoxygenase inhibitors co-inhibit heat shock protein 90 in HCT-116 cells. ChemMedChem. 2018 Nov 24;: Authors: Hey-Hawkins E, Kuhnert R, Sárosi MB, George S, Lönnecke P, Hofmann B, Steinhilber D, Steinmann S, Schneider-Stock R, Murganic B, Mijatovic S, Maksimovic-Ivanic D Abstract 5-Lipoxygenase converts arachidonic acid to leukotrienes that are involved in inflammation and angiogenesis. The introduction of carboranes can improve the pharmacokinetic behavior of metabolically less stable pharmaceutics. We here 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 for several melanoma and colon cancer cell lines. For the colon cancer cell line HCT-116 the co-inhibition of heat shock protein 90 could be detected. PMID: 30471171 [PubMed - as supplied by publisher]
Source: ChemMedChem - Category: Chemistry Authors: Tags: ChemMedChem Source Type: research