Structure-Activity Relationship and Anticancer Profile of Second-Generation Anti-MRSA Synthetic Retinoids

Ana V. Cheng, Wooseong Kim, Iliana E. Escobar, Eleftherios Mylonakis, William M. Wuest

Research output: Contribution to journalArticlepeer-review

6 Scopus citations

Abstract

We previously reported the antibacterial activity of CD437, a known antitumor compound. It proved to be a potent antimicrobial agent effective against both growing and persister cells of methicillin-resistant Staphylococcus aureus (MRSA). Herein, we report the synthesis of a panel of analogs and their effect on both MRSA and cancer cells. The hydrophobic group of the parent compound was varied in steric bulk, and lipid-mimicking analogs were tested. Biological assessment confirmed that the adamantane moiety is the most effective substitution for antibacterial activity, and some preferential action in cancer over MRSA was achieved.

Original languageEnglish
Pages (from-to)393-397
Number of pages5
JournalACS Medicinal Chemistry Letters
Volume11
Issue number3
DOIs
StatePublished - 12 Mar 2020

Keywords

  • cancer
  • CD437
  • Methicillin resistant Staphylococcus aureus
  • persister
  • retinoid

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