In vitro cytostatic activity of some amino acid 4-N-substituted cytosines.
Cytotoxicity of 22 amino acid 4-N-substituted cytosine derivatives was studied on KB and HeLa human tissue cultures. A 4-N-(1H-2-oxo-4 pyrimidyl)-tryptamine with ED50 activity values of 0.145 x 10(-3) mole/l and ED0 = 0.4 x 10(-5) mole/l showed the highest cytotoxic activity and was qualified for further in vivo investigation. The secondary modification of tryptamine substituent seems to be a determining factor of the cytotoxic activity of 4-N-pyrimidinyl amino acids. The activity of the investigated compounds was inversely dependent on their solubility limited by the results of the solubility-activity relationship analysis.
Hładoń
B
B
Department of Pharmacology, Medical Academy, Poznań, Poland.
Sloderbach
A
A
Radosh
P
P
Spychała
J
J
Gołankiewicz
K
K
D002455:Cell Division / Q000187:drug effects; D003596:Cytosine / Q000031:analogs & derivatives* / Q000633:toxicity; D006367:HeLa Cells / Q000187:drug effects; D006801:Humans; D007624:KB Cells / Q000187:drug effects; D015394:Molecular Structure; D012995:Solubility; D013329:Structure-Activity Relationship
D003596:Cytosine