Tailored α-methylene-γ-butyrolactones and their effects on growth suppression in pancreatic carcinoma cells

P. Veeraraghavan Ramachandran, Debarshi Pratihar, Hari Narayanan G. Nair, Matthew Walters, Sadie Smith, Michele T. Yip-Schneider, Huangbing Wu, C. Max Schmidt

Research output: Contribution to journalArticle

19 Scopus citations

Abstract

A selected series of racemic α-methylene-γ-butyrolactones (AMGBL) were synthesized via allylboration and screened against three human pancreatic cancer cell lines (Panc-1, MIA PaCa-2, and BxPC-3). This systematic study established a discernible relationship between the substitution pattern of AMGBL and their anti-proliferative activity. β,γ-diaryl-AMGBLs, particularly those with a trans-relationship exhibited higher potency than parthenolide and LC-1 against all three cell lines.

Original languageEnglish (US)
Pages (from-to)6620-6623
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number22
DOIs
StatePublished - Nov 15 2010

Keywords

  • Allylboration
  • Alpha-methylene-gamma-butyrolactones
  • Anti-proliferation
  • Pancreatic cancer
  • Parthenolide

ASJC Scopus subject areas

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

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