Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones

Young Woo Kim, John C. Hackett, Robert W. Brueggemeier

Research output: Contribution to journalArticlepeer-review

102 Scopus citations

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.

Original languageEnglish
Pages (from-to)4032-4040
Number of pages9
JournalJournal of Medicinal Chemistry
Volume47
Issue number16
DOIs
StatePublished - 29 Jul 2004

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