Synthesis and structure-activity studies of the V-ATPase inhibitor saliphenylhalamide (SaliPhe) and simplified analogs

Jose Garcia-Rodriguez, Saurabh Mendiratta, Michael A. White, Xiao Song Xie, Jef K. De Brabander

Research output: Contribution to journalArticlepeer-review

4 Scopus citations

Abstract

An efficient total synthesis of the potent V-ATPase inhibitor saliphenylhalamide (SaliPhe), a synthetic variant of the natural product salicylihalamide A (SaliA), has been accomplished aimed at facilitating the development of SaliPhe as an anticancer and antiviral agent. This new approach enabled facile access to derivatives for structure-activity relationship studies, leading to simplified analogs that maintain SaliPhe's biological properties. These studies will provide a solid foundation for the continued evaluation of SaliPhe and analogs as potential anticancer and antiviral agents.

Original languageEnglish (US)
Pages (from-to)4393-4398
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume25
Issue number20
DOIs
StatePublished - Jul 30 2015

Keywords

  • Anticancer
  • Antiviral
  • Benzolactone
  • Salicylihalamide
  • V-ATPase

ASJC Scopus subject areas

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

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