TY - JOUR
T1 - Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones
AU - Kim, Young Woo
AU - Hackett, John C.
AU - Brueggemeier, Robert W.
PY - 2004/7/29
Y1 - 2004/7/29
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=3242794236&partnerID=8YFLogxK
U2 - 10.1021/jm0306024
DO - 10.1021/jm0306024
M3 - Article
C2 - 15267241
AN - SCOPUS:3242794236
SN - 0022-2623
VL - 47
SP - 4032
EP - 4040
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 16
ER -