Development of 6H-chromeno[3,4-c]pyrido[3′,2′:4,5]thieno[2,3-e]pyridazin-6-ones as Par-4 secretagogues

Mykhaylo S. Frasinyuk, Svitlana P. Bondarenko, Vitaliy M. Sviripa, Ravshan Burikhanov, Vivek M. Rangnekar, Chunming Liu, David S. Watt

Research output: Contribution to journalArticlepeer-review

5 Scopus citations

Abstract

Nitrosation and cyclization of 4-(3-aminothieno[2,3-b]pyridine-2-yl)-2H-chromen-2-ones 1 afforded substituted 6H-chromeno[3,4-c]pyrido[3′,2′:4,5]thieno[2,3-e]pyridazin-6-ones 2 that inhibited the intermediary filament protein, vimentin, at low micromolar concentrations. This inhibition promoted the secretion of Prostate Apoptosis Response-4 protein (Par-4), which selectively triggered apoptosis in prostate cancer cells such as CWR22Rv1, LNCaP-derivative C4-2B, PC-3 and its aggressive analog, PC-3 MM2.

Original languageEnglish
Pages (from-to)3382-3384
Number of pages3
JournalTetrahedron Letters
Volume56
Issue number23
DOIs
StatePublished - May 25 2015

Bibliographical note

Publisher Copyright:
© 2015 Elsevier Ltd. All rights reserved.

Keywords

  • Coumarin
  • Par-4
  • Prostate Apoptosis Response-4 protein
  • Prostate cancer
  • Pyridazine
  • Vimentin

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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