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


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.

SUBMITTER: Cheng AV 

PROVIDER: S-EPMC7074213 | biostudies-literature | 2020 Mar

REPOSITORIES: biostudies-literature

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

Cheng Ana V AV   Kim Wooseong W   Escobar Iliana E IE   Mylonakis Eleftherios E   Wuest William M WM  

ACS medicinal chemistry letters 20190717 3


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 <i>Staphylococcus aureus</i> (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 th  ...[more]

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