Quinoline and thiazolopyridine allosteric inhibitors of MALT1

David A. Scott, John M. Hatcher, Hongyan Liu, Mingpeng Fu, Guangyan Du, Lorena Fontán, Ilkay Us, Gabriella Casalena, Qi Qiao, Hao Wu, Ari Melnick, Nathanael S. Gray

Research output: Contribution to journalArticlepeer-review

4 Scopus citations

Abstract

Quinolines and thiazolopyridines were developed as allosteric inhibitors of MALT1, with good cellular potency and exquisite selectivity. Mouse pharmacokinetic (PK) profiling showed these to have low in vivo clearance, and moderate oral exposure. The thiazolopyridines were less lipophilic than the quinolines, and one thiazolopyridine example was active in our hIL10 mouse pharmacodynamic (PD) model upon oral dosing.

Original languageEnglish (US)
Pages (from-to)1694-1698
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume29
Issue number14
DOIs
StatePublished - Jul 15 2019
Externally publishedYes

Keywords

  • Allosteric
  • B-cell lymphomas
  • MALT1
  • Protease inhibitors

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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