2009
DOI: 10.1002/ejoc.200801290
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Towards a New SPE Material for EDCs: Fully Automated Synthesis of a Library of Tripodal Receptors Followed by Fast Screening by Affinity LC

Abstract: A series of human estrogen receptor (hER) mimics were synthesised. On the basis of the knowledge on the structure of the hormone binding domain of the hER, three different peptide chains were constructed onto a tripodal scaffold. By using a fully automated solid-phase synthesis protocol, 120 members with known identity were synthesised in only a week. Affinity towards estrogenic compounds was checked by affinity LC. For this purpose, ethinylestradiol was "clicked" onto a modified-silica phase, and the obtained… Show more

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Cited by 11 publications
(5 citation statements)
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“…Furthermore, we have recently reported on the development of a library of EDCs-receptors based on a flexible tripodal scaffold. 10 However, no strong EDC affinity could be confirmed.…”
Section: Scaffold Considerations: From a Flexible To A Rigid Multipodmentioning
confidence: 96%
“…Furthermore, we have recently reported on the development of a library of EDCs-receptors based on a flexible tripodal scaffold. 10 However, no strong EDC affinity could be confirmed.…”
Section: Scaffold Considerations: From a Flexible To A Rigid Multipodmentioning
confidence: 96%
“…Coupling of an amino acid on a resin carrying -NH 2 groups (Scheme 1) can be completed in less than 1h at room temperature [370] thanks to various efficient catalysts [371] developed over decades. This chemistry is certainly as efficient as any well accepted click reaction.…”
Section: Coupling Strategies Of Solid Phase Peptide Synthesismentioning
confidence: 99%
“…The synthesis is based on the procedures described previously for estradiol and testosterone click stationary phases [14] .…”
Section: Synthesis Of the Stationary Phasesmentioning
confidence: 99%
“…We recently described the synthesis by click chemistry of estradiol and testosterone phases for affinity LC of tripodal receptors [14] .…”
Section: Introductionmentioning
confidence: 99%