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

Brucoli, Federico, Natoli, Antonino, Marimuthu, Preethi, Borrello, Maria Teresa, Stapleton, Paul, Gibbons, Simon and Schätzlein, Andreas (2012) Efficient synthesis and biological evaluation of proximicins A, B and C. Bioorganic and Medicinal Chemistry, 20 (6). pp. 2019-2024. ISSN 0968-0896

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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.

Item Type: Article
Uncontrolled Keywords: antibiotics,anticancer molecules,copper-catalysed amidation,distamycin and netropsin,dna-minor groove binding agents,biochemistry,molecular medicine,molecular biology,pharmaceutical science,drug discovery,clinical biochemistry,organic chemistry ,/dk/atira/pure/subjectarea/asjc/1300/1303
Faculty \ School: Faculty of Science > School of Pharmacy
Related URLs:
Depositing User: LivePure Connector
Date Deposited: 15 Jul 2020 23:39
Last Modified: 15 Jul 2020 23:39
URI: https://ueaeprints.uea.ac.uk/id/eprint/76107
DOI: 10.1016/j.bmc.2012.01.043

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