Synthesis of new amino acid and peptide derivatives of estradiol and their binding affinities for the estrogen receptor.

Abstract

A series of amino acid and peptide derivatives of estradiol have been synthesized by coupling 17 beta-aminoestra-1,3,5(10)-trien-3-ol, 17-hydrazonoestra-1,3,5(10)-trien-3-ol with amino acids or peptides, using tetrahydrothiazole-2-thione, N-hydroxy-1,4-epoxycyclohex-5-ene-2,3-dicarbonylimide, benzotriazolyloxy-tris(dimethylamino)phosphonium hexafluorophosphate, and p-nitrophenol as reagents. N-protected peptidyl steroids were deprotected by traditional methods. The relative binding affinities of the deprotected derivatives to the estrogen receptor were determined by competitive radioligand binding assay.

Cite this paper

@article{Ye1993SynthesisON, title={Synthesis of new amino acid and peptide derivatives of estradiol and their binding affinities for the estrogen receptor.}, author={Yu Ye and Yue Huang and Z Wang and S . M . Chen and Ye Tian}, journal={Steroids}, year={1993}, volume={58 1}, pages={35-9} }