2- and 3-[(Aryl)(azolyl)methyl]indoles as Potential Non-steroidal Aromatase Inhibitors.

The present study was designed to follow our pharma-comodulation work in the field of non-steroidal aromatase inhibitors. All target compounds 12a-h and 28a-h were tested in vitro for human placental aroma-tase inhibition, using testosterone or androstenedione the substrate for the aromatase enzyme and the IC30 and relative potency to aminoglutethimide data are included. A SAR study indicated that 3-[(4-fluorophenyl)(1 Himidazol-1-yl) methyl]-1-ethyl-2-methyl-1H-indole (28g) was a highly potent and selective aromatase inhibitor with IC50 value of 0.025 µM. 28 g was also a weak inhibitor of androstenedione synthesis. [ABSTRACT FROM AUTHOR]