Design, synthesis, and biological evaluation of ellipticine-estradiol conjugates

…, JA Fernandez, JA Katzenellenbogen…

Index: Devraj, Rajesh; Barrett, John F.; Fernandez, Jeffrey A.; Katzenellenbogen, John A.; Cushman, Mark Journal of Medicinal Chemistry, 1996 , vol. 39, # 17 p. 3367 - 3374

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Citation Number: 58

Abstract

Three ellipticine-estradiol conjugates were synthesized in an effort to target the cytotoxicity of ellipticine to estrogen-receptor positive cells. The three conjugates were prepared with linker chains extending from the 17α position of the estradiol to N-2 (compound 3), N-6 (compound 4), and C-9 (compound 5) positions of ellipticine. The ellipticine-estradiol conjugates were evaluated for their abilities to bind to estrogen receptors, to inhibit ...