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Synthesis and biological activities of indolocarbazoles bearing amino acid residues

2001; Elsevier BV; Volume: 36; Issue: 11-12 Linguagem: Inglês

10.1016/s0223-5234(01)01284-3

1768-3254

Pascale Moreau, Martine Sancelme, Christian Bailly, Stéphane Léonce, Alain St. Pierre, John A. Hickman, Bruno Pfeiffer, Michelle Prudhomme,

Microbial Natural Products and Biosynthesis

Three indolocarbazole compounds bearing a tripeptide or a lysine group attached to one of the indole nitrogens via a propylamino chain and two rebeccamycin derivatives bearing a lysine residue on the sugar moiety were synthesised with the aim of improving the binding to DNA and the antiproliferative activities. Four tumour cell lines, from murine L1210 leukemia, human HT29 colon carcinoma, A549 non-small cell lung carcinoma and K-562 leukemia, were used to evaluate the cytotoxicity of the drugs. Their effects on the cell cycle of L1210 cells and their antimicrobial properties against two Gram-positive bacteria Bacillus cereus and Streptomyces chartreusis, a Gram-negative bacterium Escherichia coli and a yeast Candida albicans were also investigated.