The use of the substrate-heme complex approach in the design, synthesis, biochemical evaluation, and rationalization of the inhibitory activity of a range of azole compounds against cholesterol side chain cleavage enzyme.

Here, we report the synthesis and biochemical evaluation of a number of compounds as potent inhibitors of cytochrome P450 enzymes, such as aromatase (AR), but not cholesterol side chain cleavage (CSCC). This is a crucial enzyme in the steroidal cascade and its inhibition results in major side-effects, as a result, the ability of compounds to specifically inhibit enzymes such as AR but not CSCC would be an important factor in the drug design process.