Cloridarol aromatase inhibitor

[Smyth2]

I was checking through my files and found an agent made from Cloridarol which has 97.4 times the potency of aminoglutethimide as an aromatase inhibitor.

Vinh, T.K.; Ahmadi, M.; Lopez Delgado, P.O.; Fernandez Perez, S.; Walters, H.M.; Smith, H.J.; Nicholls, P.J.; Simons, C. (1999). "1-[(Benzofuran-2-yl)phenylmethyl]-triazoles and -tetrazoles - potent competitive inhibitors of aromatase". Bioorganic & Medicinal Chemistry Letters. 9 (14): 2105–2108. doi:10.1016/S0960-894X(99)00328-5.

 

[polymath]

That's not the same molecule as the one in the Wikipedia article. The one there doesn't have that ring with 4 nitrogen atoms, which I suppose is necessary for aromatase inhibiting activity as letrozole also has a multiple nitrogen ring.

 

[Voxide]

which has 97.4 times the potency of aminoglutethimide as an

There’s one I haven’t heard in a while
, glad it phased out and replaced with better options. Testolactone was another one

If this is any more potent than letro, sounds like a great way to crash your estrogen and make your life miserable. A lotta this stuff is cool on paper and in a lab but serves zero purpose in your actual body

 

[4DQSAR]

There’s one I haven’t heard in a while
, glad it phased out and replaced with better options. Testolactone was another one

If this is any more potent than letro, sounds like a great way to crash your estrogen and make your life miserable. A lotta this stuff is cool on paper and in a lab but serves zero purpose in your actual body

In vitro models can do a spectacularly bad job of demonstating how a drug acts in vivo. Even animal models can be surprisingly poor.

I've seen compounds where every single metric suggested them to be highly potent only for the animal models to show them no more potent than the parent drug. Of course, those were not human models, but it's important to realize that while useful in early testing, whatever you have is only as good as it's in vivo activity in the species it's intended for.