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.
Recommended Citation
Su, Bin; Hackett, John C.; Diaz-Cruz, Edgar S.; Kim, Young Woo; and Brueggemeier, Robert W., "Lead Optimization of 7-benzyloxy 2-(4′-pyridylmethyl)Thio Isoflavone Aromatase Inhibitors" (2005). Chemistry Faculty Publications. 399.
https://engagedscholarship.csuohio.edu/scichem_facpub/399
Creative Commons License
This work is licensed under a Creative Commons Attribution-NonCommercial-No Derivative Works 4.0 International License.
DOI
10.1016/j.bmc.2005.07.038
Version
Postprint
Volume
13
Issue
23
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.).