Design and evaluation of fragment-like estrogen receptor tetrahydriosoquinoline ligand from a scaffold-detection approach

S. Möcklinghoff, W.A.L. Otterlo, van, R. Rose, S. Fuchs, T.J. Zimmermann, M.D. Seoane, H. Waldmann, C. Ottmann, L. Brunsveld

Research output: Contribution to journalArticleAcademicpeer-review

13 Citations (Scopus)

Abstract

A library of small tetrahydroisoquinoline ligands, previously identified via structure- and chemistry-based hierarchical organization of library scaffolds in tree-like arrangements, has been generated as novel estrogen receptor agonistic fragments via traditional medicinal chemistry exploration. The approach described has allowed for the rapid evaluation of a structure-activity relationship of the ligands concerning estrogen receptor affinity and estrogen receptor ß subtype selectivity. The structural biological insights obtained from the fragments aid the understanding of larger analogues and constitute attractive starting points for further optimization.
Original languageEnglish
Pages (from-to)2005-2011
JournalJournal of Medicinal Chemistry
Volume54
Issue number7
DOIs
Publication statusPublished - 2011

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