O

FIGURE 3.20 Interaction of fradozole with the aromatase active site.

C=N Ser-478

FIGURE 3.20 Interaction of fradozole with the aromatase active site.

The third generation of nonsteroidal aromatase inhibitors includes the triazole derivatives anastrozole, vorozole, and letrozole, which are very potent and specific aromatase inhibitors that allow almost complete estrogen suppression.32 They have the advantage over aminoglutethimide and fadrozole of not showing affinity for other cytochrome P450-related steroidogenic enzymes because the presence of two electron-withdrawing nitrogen atoms in the triazole ring renders it too electron-deficient for aromatic oxidation. The related triazole derivative finrazole, another selective aromatase inhibitor, is under clinical studies for the treatment of male lower urinary dysfunction, a hitherto intractable disease.

10 Ways To Fight Off Cancer

10 Ways To Fight Off Cancer

Learning About 10 Ways Fight Off Cancer Can Have Amazing Benefits For Your Life The Best Tips On How To Keep This Killer At Bay Discovering that you or a loved one has cancer can be utterly terrifying. All the same, once you comprehend the causes of cancer and learn how to reverse those causes, you or your loved one may have more than a fighting chance of beating out cancer.

Get My Free Ebook


Post a comment