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Antimicrobial and antineoplastic activities of Agelasine analogs modified in the purine 2-position
Department of Chemistry, Oslo University.
Faculty of Health Sciences, Oslo University.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Pharmacognosy.
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2011 (English)In: Archiv der Pharmazie, ISSN 0365-6233, E-ISSN 1521-4184, Vol. 344, no 1, 50-55 p.Article in journal (Refereed) Published
Abstract [en]

Agelasines are 7,9-dialkylpurinium salts found in marine sponges (Agelas sp.), which display a variety of antimicrobial and cytotoxic effects. We have synthesized simplified agelasine analogs modified in the purine 2-position and examined their antimicrobial and anticancer activities. The compounds were screened against Staphylococcus aureus, Escherichia coli, Mycobacterium tuberculosis, Candida krusei, and Candida albicans, protozoa causing tropical diseases (Plasmodium falciparum, Leishmania infantum, Trypanosoma cruzi, and Trypanosoma brucei), a panel of human cancer cell lines (U-937 GTB, RPMI 8226/s, CEM/s, and ACHN) as well as VERO and/or MRC-5 cells. The results indicate that the introduction of a methyl group in the purine 2-position is beneficial for antimycobacterial and antiprotozoal activity, and that amino groups may enhance activity against several cancer cell lines.

Place, publisher, year, edition, pages
2011. Vol. 344, no 1, 50-55 p.
Keyword [en]
Agelasine, Antibacterial activity, Anticancer acivitity, Antifungal activity, Antiprotozoal activity
National Category
Pharmaceutical Sciences
Identifiers
URN: urn:nbn:se:uu:diva-141123DOI: 10.1002/ardp.201000148ISI: 000287004600005PubMedID: 21213351OAI: oai:DiVA.org:uu-141123DiVA: diva2:385155
Available from: 2011-01-11 Created: 2011-01-11 Last updated: 2017-12-11Bibliographically approved

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Larsson, RolfBohlin, Lars

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