Structure-activity relationship studies on selected iso-alpha-carbolines. I.
In the course of microbial transformation of the antitumor compounds, it has been found that iso-alpha-carbolines and their certain derivatives undergo N-1 methylation by Kitasatosporia setae. The resulting products, iso-alpha-carbolines exhibit antibacterial and antifungal properties in the concentration range of 0.2-2.5 mumol/ml. In the cytotoxicity test only derivatives substituted at C-2 and C-4 display moderate activity against KB cells. None of the compounds tested show a significant inhibitory effect against P388 lymphocytic leukemia.
Peczyńska-Czoch
W
W
Mordarski
M
M
Kaczmarek
L
L
Nantka-Namirski
P
P
D000192:Actinomycetales / Q000187:drug effects; D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D000935:Antifungal Agents / Q000494:pharmacology*; D002243:Carbolines / Q000494:pharmacology* / Q000627:therapeutic use; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D007624:KB Cells; D007941:Leukemia P388 / Q000188:drug therapy; D008297:Male; D051379:Mice; D008811:Mice, Inbred DBA; D008826:Microbial Sensitivity Tests; D008837:Micrococcus / Q000187:drug effects; D012441:Saccharomyces cerevisiae / Q000187:drug effects; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D002243:Carbolines