Abstract
A series of 1-[(benzofuran-2-yl) phenylmethyl] imidazoles have been evaluated as inhibitors of microsomal 17α-hydroxylase: 17, 20-lyase (P450 17) from rat and human testes, and bovine adrenals. Ketoconazole has 110-fold selectivity for the human enzyme. This selectivity was mirrored in several equipotent imidazole derivatives. Some compounds, although potent inhibitors of the human enzyme, were less effective against the rat enzyme. This demonstrates the need to screen candidate inhibitors, intended as agents for the treatment of prostatic cancer, against the human enzyme.
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