Document Type

Article

Publication Date

12-1-2005

Publication Title

Bioorganic & Medicinal Chemistry

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 IC50 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.

Comments

This research was supported by NIH Grant CA73698 (R.W.B.), USAMRMC Breast Cancer Program Idea Grant DMAD-17-00-1-0388 (R.W.B.), and USAMRMC Breast Cancer Program Predoctoral Fellowships DMAD17-02-1-0529 (J.C.H.) and DMAD17-99-1-9342 (Y.W.K.).

Creative Commons License

Creative Commons Attribution-Noncommercial-No Derivative Works 4.0 License
This work is licensed under a Creative Commons Attribution-Noncommercial-No Derivative Works 4.0 License.

DOI

10.1016/j.bmc.2005.07.038

Version

Postprint

Volume

13

Issue

23

Included in

Chemistry Commons

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