Chemically reactive estrogens: synthesis and estrogen receptor interactions of hexestrol ether derivatives and 4-substituted deoxyhexestrol derivatives bearing alkylating functions

• Published in: Journal of medicinal chemistry Vol. 24; no. 4; pp. 435 - 450
• Main Authors: Katzenellenbogen, John A, McGorrin, Robert J, Tatee, Tochiro, Kempton, Robert J, Carlson, Kathryn E, Kinder, David H
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 01.04.1981
• Subjects: Affinity Labels - pharmacology; Alkylating Agents - chemical synthesis; Alkylating Agents - pharmacology; Binding Sites; Estrogens - chemical synthesis; Estrogens - metabolism; Estrogens - pharmacology; Hexestrol - chemical synthesis; Hexestrol - metabolism; Photolysis; Receptors, Estrogen - drug effects; Receptors, Estrogen - metabolism; Structure-Activity Relationship

A series of chemically reactive derivatives of the nonsteroidal estrogen hexestrol have been synthesized as potential affinity labels for the estrogen receptor or as cytotoxic agents with selective activity against receptor-containing cells. These compounds are hexestrol ethers with halo ketone, hal...