Antimicrobial and antineoplastic activities of agelasine analogs modified in the purine 2-position.

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.
AuthorsHeidi Roggen, Colin Charnock, Robert Burman, Jenny Felth, Rolf Larsson, Lars Bohlin, Lise-Lotte Gundersen
JournalArchiv der Pharmazie (Arch Pharm (Weinheim)) Vol. 344 Issue 1 Pg. 50-5 (Jan 2011) ISSN: 1521-4184 [Electronic] Germany
PMID21213351 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Anti-Bacterial Agents
  • Antifungal Agents
  • Antineoplastic Agents
  • Antiparasitic Agents
  • Purines
  • agelasine D
  • Animals
  • Anti-Bacterial Agents (chemical synthesis, chemistry, pharmacology)
  • Antifungal Agents (chemical synthesis, chemistry, pharmacology)
  • Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
  • Antiparasitic Agents (chemical synthesis, chemistry, pharmacology)
  • Cell Line
  • Cell Line, Tumor
  • Cercopithecus aethiops
  • Humans
  • Neoplasms (drug therapy, pathology)
  • Purines (chemical synthesis, chemistry, pharmacology)
  • Structure-Activity Relationship
  • Vero Cells

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