Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones.

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Kim YW, Hackett JC, Brueggemeier RW

Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones.

J Med Chem. 2004 Jul 29;47(16):4032-40.

PubMed ID

15267241 [ View in PubMed

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Abstract

Aromatase, a cytochrome P450 hemoprotein that is responsible for estrogen biosynthesis by conversion of androgens into estrogens, has been an attractive target in the treatment of hormone-dependent breast cancer. As a result, a number of synthetic steroidal or nonsteroidal aromatase inhibitors have been successfully developed. In addition, there are several classes of natural products that exert potent activities in aromatase inhibition, with the flavonoids being most prominent. Previous studies have exploited flavone and flavanone scaffolds for the development of new aromatase inhibitors. In this paper, we describe the design, synthesis, and biological evaluation of a novel series of 2-(4'-pyridylmethyl)thioisoflavones as the first example of synthetic isoflavone-based aromatase inhibitors.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Aminoglutethimide	Cytochrome P450 19A1	Ki (nM)	1410	7	37	Details
Aminoglutethimide	Cytochrome P450 19A1	IC 50 (nM)	2800	7	37	Details