Carborane-Based Analogues of 5-Lipoxygenase Inhibitors Co-inhibit Heat Shock Protein 90 in HCT116 Cells.
2018
Authors:
Kuhnert, RobertSárosi, Menyhárt-Botond
George, Sven
Lönnecke, Peter
Hofmann, Bettina
Steinhilber, Dieter
Steinmann, Sara
Schneider-Stock, Regine
Murganić, Blagoje
Mijatović, Sanja
Maksimović-Ivanić, Danijela
Hey-Hawkins, Evamarie
Document Type:
Article (Accepted Version)
,
© 2018 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim
Metadata
Show full item recordAbstract:
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.
Keywords:
Cancer; Carboranes; Heat shock protein 90; Inhibitors; LipoxygenaseSource:
ChemMedChem, 2018Funding / projects:
- Molecular mechanisms of physiological and pharmacological control of inflammation and cancer (RS-MESTD-Basic Research (BR or ON)-173013)
- DFG. Grant Numbers: SFB 1039, HE 1376/38-1, SA 2902/2-1
DOI: 10.1002/cmdc.201800651
PubMed: 30471171