Owen, Caroline P, Dhanani, Sachin, Patel, Chirag H, Shahid, Imran and Ahmed, Sabbir (2006) Synthesis and biochemical evaluation of a range of potent benzyl imidazole-based compounds as potential inhibitors of the enzyme complex 17[alpha]-hydroxylase/17,20-lyase (P450[sub]17[alpha]). Bioorganic & Medicinal Chemistry Letters, 16(15), pp. 4011-4015. ISSN (print) 0960-894X
Full text not available from this archive.Abstract
The cytochrome P-450 enzyme, 17alpha-hydroxylase/17,20-lyase (P450(17alpha)), is a potential target in hormone-dependent cancers. Here, we report the synthesis and biochemical evaluation of a range of benzyl imidazole-based compounds which have been targeted against the two components of this enzyme, that is, 17alpha-hydroxylase (17alpha-OHase) and 17,20-lyase (lyase). The results from the biochemical testing suggest that the compounds synthesised are good inhibitors, with N-4-iodobenzyl imidazole (5) (IC50=10.06 microM against 17alpha-OHase and IC50=1.58 microM against lyase) showing equipotent activity against lyase compared to the standard compound, ketoconazole (KTZ) (IC50=3.76+/-0.01 microM against 17alpha-OHase and IC50=1.66+/-0.15 microM against lyase). Furthermore, the compounds tested are less potent towards the 17alpha-OHase component, a desirable property in the development of novel inhibitors of P450(17alpha).
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | lyase, hydroxylase, p-45017 alpha, inhibitors, substrate-haem complex, prostate-cancer, chemotherapy, target |
| Research Area: | Chemistry Biological sciences |
| Faculty, School or Research Centre: | Faculty of Science (until 2011) > School of Life Sciences Faculty of Science (until 2011) > School of Pharmacy and Chemistry |
| Related URLs: | |
| Depositing User: | Automatic Import Agent |
| Date Deposited: | 25 Feb 2010 12:06 |
| Last Modified: | 02 Dec 2011 16:04 |
| URI: | http://eprints.kingston.ac.uk/id/eprint/7080 |
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