Synthesis and cytotoxicity of new potential intercalators based on tricyclic systems of some pyrimido[5,4-c]cinnoline and pyrimido[5,4-c]quinoline derivatives. Part I.
Pyrimido[5,4-c]cinnoline and pyrimido[5,4-c]quinoline derivatives have been tested as potential intercalators. All of them embody stuctural properties alike to afford intercalating activity. Their cytotoxicity was determined on the two human leukemia cell lines, the promyelocytic HL-60 and the lymphoblastic NALM-6. The viability of cells exposed continuously to tested compounds was estimated by the trypan-blue exclusion assay. IC50 data for the NALM-6 cell line are lower than for the HL-60 cell line, what suggested that the HL-60 leukemia cells are more resistant to toxic action of tested compounds. All compounds exerted moderate cytotoxic activity. The compounds were analyzed with the HyperChem/ChemPlus software trying to find basic structure-activity relationships.
Lewgowd
Wiesława
W
Department of Pharmaceutical Chemistry and Drug Analysis, Medical University of Lódź, 1 Muszyńskiego Str., 90-151 Lódź, Poland.
Stańczak
Andrzej
A
Ochocki
Zbigniew
Z
Krajewska
Urszula
U
Rózalski
Marek
M
D001952:Bridged-Ring Compounds / Q000138:chemical synthesis* / Q000145:classification / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D018922:HL-60 Cells; D006574:Heterocyclic Compounds, 2-Ring / Q000138:chemical synthesis / Q000494:pharmacology; D006575:Heterocyclic Compounds, 3-Ring / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D007364:Intercalating Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D011724:Pyridazines / Q000138:chemical synthesis / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology; D021281:Quantitative Structure-Activity Relationship; D011804:Quinolines / Q000138:chemical synthesis / Q000494:pharmacology
D001952:Bridged-Ring Compounds; D006574:Heterocyclic Compounds, 2-Ring; D006575:Heterocyclic Compounds, 3-Ring; D007364:Intercalating Agents; D011724:Pyridazines; D011743:Pyrimidines; D011804:Quinolines; C509496:pyrimido(5,4-c)cinnoline; C476282:cinnoline