proximicin-b and Bacterial-Infections

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.

Topics: Anti-Bacterial Agents; Antibiotics, Antineoplastic; Apoptosis; Bacterial Infections; Cell Line, Tumor; Enterococcus faecalis; Escherichia coli; Female; Humans; Methicillin-Resistant Staphylococcus aureus; Microbial Sensitivity Tests; Neoplasms; Netropsin; Staphylococcus aureus