Lead optimization of 7-benzyloxy 2-(4'-pyridylmethyl)thio isoflavone aromatase inhibitors.

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Su B, Hackett JC, Diaz-Cruz ES, Kim YW, Brueggemeier RW

Lead optimization of 7-benzyloxy 2-(4'-pyridylmethyl)thio isoflavone aromatase inhibitors.

Bioorg Med Chem. 2005 Dec 1;13(23):6571-7. Epub 2005 Aug 24.

PubMed ID
16125392 [ View in PubMed
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Abstract

Aromatase, the enzyme responsible for estrogen biosynthesis, is a particularly attractive target in the treatment of hormone-dependent breast cancer. The synthesis and biological evaluation of a series of 2-(4'-pyridylmethyl)thio, 7-alkyl- or aryl-substituted isoflavones as potential aromatase inhibitors are described. The isoflavone derivatives demonstrate IC(50) values from 79 to 553 nM and compete with the endogenous substrate, androstenedione. Data supporting the ability of these analogs to suppress aromatase enzyme activity in the SK-BR-3 breast cancer cell line are also presented.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
AminoglutethimideCytochrome P450 19A1Ki (nM)1410737Details
AminoglutethimideCytochrome P450 19A1IC 50 (nM)2800737Details