New selective nonsteroidal aromatase inhibitors: Synthesis and inhibitory activity of 2, 3 or 5-(α-azolylbenzyl)-1H-indoles

Article abstract of DOI:10.1016/S0960-894X(98)00737-9

Six azolyl substituted indoles were synthesized and tested for their activity to inhibit two P450 enzymes: P450 arom and P450 17α. It was observed that the introduction of α-imidazolylbenzyl chain at carbon 3 or 5 on indole nucleus led to very active molecules. Compounds 22, 23 and especially 33 demonstrate very high potential against P450 arom. Under our assay conditions of high substrate concentration the IC₅₀ are 0.057, 0.0785 and 0.041 μM, respectively. These compounds are moderate inhibitors against P450 17α.