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Antimicrobial and Antineoplastic Activities of Agelasine Analogs Modified in the Purine 2‐Position
Author(s) -
Roggen Heidi,
Charnock Colin,
Burman Robert,
Felth Jenny,
Larsson Rolf,
Bohlin Lars,
Gundersen LiseLotte
Publication year - 2011
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201000148
Subject(s) - antimicrobial , antimycobacterial , antiprotozoal , candida albicans , trypanosoma cruzi , leishmania infantum , microbiology and biotechnology , antiparasitic , staphylococcus aureus , biology , plasmodium falciparum , purine analogue , mycobacterium tuberculosis , purine , chemistry , biochemistry , leishmaniasis , bacteria , tuberculosis , medicine , immunology , in vitro , parasite hosting , malaria , enzyme , pathology , world wide web , computer science , genetics , visceral leishmaniasis
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.