A Review of Coumarin Derivatives in Pharmacotherapy of Breast Cancer
October 2008
in “
Current Medicinal Chemistry
”
TLDR Coumarin derivatives show promise as anti-estrogenic agents for treating breast cancer, with some in clinical trials.
The 2008 document reviews the potential of coumarin derivatives in breast cancer treatment, highlighting their roles as steroid sulfatase inhibitors, aromatase inhibitors, and selective estrogen receptor modulators. It discusses the structure-activity relationship of these compounds, their interactions with estrogen receptors, and the synthetic methods for creating pharmacologically significant analogs. The review emphasizes the importance of the coumarin ring system in developing new therapeutic agents for breast cancer. It also examines the efficacy of FDA-approved aromatase inhibitors and the antiproliferative activity of coumarin-estrogen conjugates in various breast cancer cell lines, with conjugate 49 showing the highest activity against MDA-MB-435 lines. The document concludes that coumarin derivatives are being investigated as anti-estrogenic agents for breast cancer treatment, with some currently in clinical trials, supported by NIH grants.
