Novel SAR for quinazoline inhibitors of EHMT1 and EHMT2

Ruben Leenders, Remco Zijlmans, Bart van Bree, Marc van de Sande, Federica Trivarelli, Eddy Damen, Anita Wegert, Daniel Müller, Jan Erik Ehlert, Daniel Feger, Carolin Heidemann-Dinger, Michael Kubbutat, Christoph Schächtele, Danny C Lenstra, Jasmin Mecinović, Gerhard Müller

Research output: Contribution to journalJournal articleResearchpeer-review

Abstract

Detailed structure activity relationship of two series of quinazoline EHMT1/EHMT2 inhibitors (UNC0224 and UNC0638) have been elaborated. New and active alternatives are presented for the ubiquitous substitution patterns found in literature for the linker to the lysine mimicking region and the lysine mimic itself. These findings could allow for advancing EHMT1/EHMT2 inhibitors of that type beyond tool compounds by fine-tuning physicochemical properties making these inhibitors more drug-like. .

Original languageEnglish
JournalBioorganic & Medicinal Chemistry Letters
Volume29
Issue number17
Pages (from-to)2516-2524
Number of pages9
ISSN0960-894X
DOIs
Publication statusPublished - Sept 2019
Externally publishedYes

Bibliographical note

Copyright © 2019 Elsevier Ltd. All rights reserved.

Keywords

  • EHMT1
  • EHMT2
  • Epigenetics
  • Histone Lysine Methyl Transferase (HMKT)
  • ONQXWOCNSKDACO-UHFFFAOYSA-N
  • Quinazoline
  • ZDINBSHEURZXDD-UHFFFAOYSA-N

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