Tricyclic thiazoles are a new class of angiogenesis inhibitors

Shridhar Bhat, Joong Sup Shim, Jun O. Liu

Research output: Contribution to journalArticlepeer-review

Abstract

Tricyclic thiazoleamine derivatives that were identified as hits in a screen against human umbilical vein endothelial cell proliferation were subjected to a structure-activity relationship study. Two structurally superimposable scaffolds - 4H-thiochromeno[4,3-d]thiazol-2-amine and 5,6-dihydro-4H-benzo[6,7]cyclohepta[1,2-d]thiazol-2-amine derivatives - yielded low-micromolar inhibitors, and two among them 37 and 43 also exhibited antiangiogenic activity in an endothelial tube formation assay. Thus, 37 and 43 can serve as leads to develop a novel class of antiangiogenic agents.

Original languageEnglish (US)
Pages (from-to)2733-2737
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number9
DOIs
StatePublished - May 1 2013

Keywords

  • Angiogenesis
  • Endothelial cells
  • Tricyclic thiazoles

ASJC Scopus subject areas

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

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