AI Article Synopsis
- Aromatase is an enzyme that converts androgens into estrogens, and targeting it could help reduce estrogen levels in breast cancer patients.
- Researchers tested several compounds derived from aminoestrones and found that isonicotinyl derivatives 5c and 10c were effective inhibitors of aromatase, with moderate potency.
- The promising results indicate that these isonicotinyl-substituted compounds can likely reach the active site of aromatase, making them potential therapeutic options.
Article Abstract
Aromatase, which is responsible for the conversion of androgens to estrogens, is a potential therapeutic target for the selective lowering estrogen level in patients with estrogen-dependent breast cancer. We prepared and tested series of the pyridine- and other heterocyclic ring-containing derivatives of 2- and 4-aminoestrones, estrone, and estradiol, compounds 5, 10, 12 and 15. The isonicotinyl derivatives of 2- and 4-aminoestrone, compounds 5c and 10c, were fairly potent competitive inhibitors of aromatase (K(i), 2.1+/-0.14 and 1.53+/-0.08 microM for 5c and 10c, respectively) and other compounds did not show, to a significant extent, the aromatase inhibitory activity. This result suggests that the isonicotinyl-substituted derivatives 5c and 10c would be accessible to the active site of aromatase.
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| http://dx.doi.org/10.1248/cpb.56.1304 | DOI Listing |
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