Synthesis, Biochemical Evaluation and Rationalisation of the Inhibitory Activity of a Range of Derivatives of 2-imidazol-1-yl-1-phenyl-ethanone as Potential Novel Inhibitors of 17α-hydroxylase/17,20-lyase (P-45017α)

Title: Synthesis, Biochemical Evaluation and Rationalisation of the Inhibitory Activity of a Range of Derivatives of 2-imidazol-1-yl-1-phenyl-ethanone as Potential Novel Inhibitors of 17α-hydroxylase/17,20-lyase (P-45017α)

Volume: 8 Issue: 6

Author(s): Kruti Shah, Baljeet Jandu, Ammara Abdullah and Sabbir Ahmed

Affiliation:

Keywords: Androgen, Enzyme inhibitor, 17α-hydroxylase, Imidazole, 17,20-lyase, Prostate cancer, Biochemical, 2-imidazol-1-yl-1-phenyl-ethanone, P-45017α, cytochrome, androstenedione (AD), dehydroepiandrosterone (DHEA), progesterone, pregnenolone, NADPH, iron-monooxygen

Abstract: We report the results of the evaluation of a series of imidazole-based compounds against the enzyme 17α- hydroxylase/17,20-lyase (P-45017α). The results show that the compounds were, in general, weak inhibitors of P-45017α in comparison to the standard inhibitor ketoconazole (KTZ) - one was, however, found to be more potent than KTZ.

Cite this article as:

Shah Kruti, Jandu Baljeet, Abdullah Ammara and Ahmed Sabbir, Synthesis, Biochemical Evaluation and Rationalisation of the Inhibitory Activity of a Range of Derivatives of 2-imidazol-1-yl-1-phenyl-ethanone as Potential Novel Inhibitors of 17α-hydroxylase/17,20-lyase (P-45017α), Letters in Drug Design & Discovery 2011; 8 (6) . https://dx.doi.org/10.2174/157018011795906749