136206-17-2Relevant articles and documents
Studies of the enzymatic synthesis of N-protected amino acid-estradiol derivatives in an organic solvent
Yan, Ai-Xin,Xing, Guo-Wen,Ye, Yun-Hua,Tian, Gui-Ling,Wong, Man-Sau,Lee, Kin-Sing
, p. 5379 - 5381 (2000)
Amino acid-estradiol derivatives were synthesized via protease-catalyzed condensation for the first time and the optimum conditions were studied systematically. (C) 2000 Elsevier Science Ltd.
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