136206-21-8Relevant articles and documents
Synthesis of new amino acid and peptide derivatives of estradiol and their binding affinities for the estrogen receptor
Ye, Yun-hua,Huang, Yun-sheng,Wang, Zhi-qing,Chen, Su-ming,Tian, Ying
, p. 35 - 39 (2007/10/02)
A series of amino acid and peptide derivatives of estradiol have been synthesized by coupling 17β-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.Keywords: 17β-aminoestradiol derivatives; 17-hydrazonoestrone derivatives; amino acids; peptides; binding affinity; estrogen receptor; steroids