Synthesis and Evaluation of 17α-E-20-(Heteroaryl)norpregn-1,3,5 (10),20-tetraene-3,17β-diols [17α-(Heteroaryl)vinyl Estradiols] as Ligands for the Estrogen Receptor-α Ligand Binding Domain (ERα-LBD).

Sandra L. Olmsted,Pakamas Tongcharoensirikul,Emmett McCaskill,Karla Gandiaga,David Labaree,Richard B. Hochberg,Robert N. Hanson

Synthesis and Evaluation of 17α-E-20-(Heteroaryl)norpregn-1,3,5 (10),20-tetraene-3,17β-diols [17α-(Heteroaryl)vinyl Estradiols] as Ligands for the Estrogen Receptor-α Ligand Binding Domain (ERα-LBD).

2012

Sandra L. Olmsted
Pakamas Tongcharoensirikul
Emmett McCaskill
Karla Gandiaga
David Labaree
Richard B. Hochberg
Robert N. Hanson

A series of 17α-(heteroaryl)vinyl estradiols (III) is synthesized to evaluate the influence of heteroatom on the affinity and efficacy of estrogenic ligands for the estrogen receptor-alpha ligand binding domain.

Keywords:

Stereochemistry
Estradiols
Ligand (biochemistry)
Heteroatom
Estrogen
Ligand
Estrogen receptor
Chemistry
Organic chemistry
ligand binding domain

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