Coumestrol has about the same binding affinity for the ER-βestrogen receptor as 17β-estradiol, but much less affinity than 17α-estradiol, although the estrogenic potency of coumestrol at both receptors is much less than that of 17β-estradiol.[4]
Because of the estrogenic activity of some coumestans, a variety of syntheses have been developed that allow the preparation of coumestans so that their pharmacological effects can be explored.[5][6]
^Singh, Rishi Pal; Singh, Daljeet (1985). "An elegant synthesis of 6H-benzofuro[3,2-c][1]benzopyran-6-ones". Heterocycles. 23 (4): 903. doi:10.3987/R-1985-04-0903 (inactive 2024-03-07).{{cite journal}}: CS1 maint: DOI inactive as of March 2024 (link)
^V. A. Tuskaev (April 2013). "Synthesis and biological activity of coumestan derivatives (Review)". Pharmaceutical Chemistry Journal. 47 (1): 1–11. doi:10.1007/s11094-013-0886-5. S2CID32550281.
^Yao, Tuanli; Yue, Dawei; Larock, Richard C (2005). "An Efficient Synthesis of Coumestrol and Coumestans by Iodocyclization and Pd-Catalyzed Intramolecular Lactonization". Journal of Organic Chemistry. 70 (24): 9985–9989. doi:10.1021/jo0517038. PMID16292831.
^Takeda, Norihiko; Miyata, Okiko; Naito, Takeaki (2007). "Efficient synthesis of benzofurans utilizing [3,3]-sigmatropic rearrangement triggered by N-trifluoroacetylation of oxime ethers: short synthesis of natural 2-arylbenzofurans". European Journal of Organic Chemistry. 2007 (9): 1491–1509. doi:10.1002/ejoc.200601001.