Synthesis and CYP24 inhibitory activity of 2-substituted-3,4-dihydro-2H-naphthalen-1-one (tetralone) derivatives

Yee, Sook Wah and Simons, Claire ORCID: https://orcid.org/0000-0002-9487-1100 2004. Synthesis and CYP24 inhibitory activity of 2-substituted-3,4-dihydro-2H-naphthalen-1-one (tetralone) derivatives. Bioorganic & Medicinal Chemistry Letters 14 (22) , pp. 5651-5654.

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Abstract

The synthesis of novel 2-benzyl- and 2-benzylidene-3,4-dihydro-2H-naphthalen-1-one (tetralone) derivatives and their inhibitoryactivity versus kidney mitochondrial 25-hydroxyvitamin D3 24-hydroxylase (CYP24) is described. The 2-benzylidenetetralone derivatives were found to be very weak inhibitors (IC50 20 >100 μM), whereas the 2-benzyltetralone derivatives showed promising inhibitoryactivity (IC50 0.9 μM for the most active derivative) compared with ketoconazole (IC50 20 μM).

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Schools > Pharmacy
Subjects:	R Medicine > RS Pharmacy and materia medica
Additional Information:	Miss Sook Wah Yee would like to acknowledge the ORS Awards Scheme for a United Kingdom Scholarship.
Last Modified:	19 Oct 2022 09:03
URI:	https://orca.cardiff.ac.uk/id/eprint/19827

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