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ChemMedChem. 2019 Jan 22;14(2):255-261. doi: 10.1002/cmdc.201800651. Epub 2018 Dec 21.

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

Author information

1
Faculty of Chemistry and Mineralogy, Institute of Inorganic Chemistry, Universität Leipzig, Johannisallee 29, 04103, Leipzig, Germany.
2
Institut für Pharmazeutische Chemie, Johann-Wolfgang-Goethe-Universität Frankfurt, Max-von-Laue-Straße 9, 60438, Frankfurt, Germany.
3
Pathologisches Institut, Universität Erlangen, Universitätsstraße 22, 91054, Erlangen, Germany.
4
Department of Immunology, Institute for Biological Research "Sinisa Stankovic", University of Belgrade, Bul. despota Stefana 142, 11060, Belgrade, Serbia.

Abstract

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; lipoxygenase

PMID:
30471171
DOI:
10.1002/cmdc.201800651

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