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Bioorg Med Chem. 2012 Mar 15;20(6):2019-24. doi: 10.1016/j.bmc.2012.01.043. Epub 2012 Feb 4.

Efficient synthesis and biological evaluation of proximicins A, B and C.

Author information

1
UCL School of Pharmacy, 29-39 Brunswick Square, London, WC1N 1AX, UK. federico.brucoli@pharmacy.ac.uk

Abstract

A quick and efficient synthesis and the biological evaluation of promising antitumor-antibiotics proximicins A, B and C are reported. The characteristic repetitive unit of these molecules, the methyl 4-Boc-aminofuran-2-carboxylate 15, was prepared in three synthetic steps in good yield using an optimised copper-catalysed amidation method. The proximicins were evaluated for their antitumor activity using cellular methods. Proximicin B induced apoptosis in both Hodgkin's lymphoma and T-cell leukemia cell lines and proximicin C exhibited significantly high cytotoxicity against glioblastoma and breast carcinoma cells. The proximicins were also screened against Escherichia coli, Enterococcus faecalis and several strains of methicillin-and multidrug-resistant Staphylococcus aureus. Proximicin B showed noteworthy activity against antibiotic-resistant Gram-positive cocci.

PMID:
22364744
DOI:
10.1016/j.bmc.2012.01.043
[Indexed for MEDLINE]

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