Evidence for new non-steroidal human aromatase inhibitors and comparison with equine aromatase inhibition for an understanding of the mammalian active site

摘要: Abstract We developed a new comparative model in order to better understand the structure-function relationships of active site human aromatase. Thus, we undertook inhibition and equine aromatases with compounds. In fact, aromatase represents only easy available mammalian membrane-bound enzyme model, besides one, which is biochemically purified, well characterized cloned. During course our work concerning synthesis screening drugs on aromatases, identified two indane derivatives inhibited (IC 50 = 3.5 μM 5.9 μM) strongly selectively while they were much less one > 10 μM). The hitherto known inhibitors, such as 4-hydroxyandrostenedione (4-OHA) some other indane-related derivatives, are equally efficient both enzymes. this work, using theoretical 3D aromatase, have explained selectivity described compounds due specific differences between primary structure sites These results could allow family that more potent selective inhibitors.