5-(2-Ethyl-phenyl)-3-(3-methoxy-phenyl)-1H-[1,2,4]triazole (DL-111-IT) and related compounds induce apoptotic patterns in cultures of human tumor cell lines.
5-(2-Ethyl-phenyl)-3-(3-methoxy-phenyl)-1H-[1,2,4]triazole (DL-111-IT) and related compounds were extensively studied as anti-gestational agents and some of these molecules were also described as inhibitors of ornithine decarboxylase. Polyamine depletion has been frequently related to the induction of apoptosis and consequently we investigated DL-111-IT and analogs for this effect in myeloid (HL60), neuroblastic (SK-N-MC) and epithelial (BeWo) human tumor cell lines, by means of electron microscopy and DNA electrophoresis. HL60 and SK-N-MC appeared notably sensitive to apoptosis, whereas BeWo responsiveness was variable and frequently associated with necrosis. Our results indicate that the contragestational effect of DL-111-IT and analogs is associated with apoptotic deletion of chorionic tissue and that these molecules, due to their effect on human tumor cell lines, can be considered as antiblastic lead compounds.
Burattini
S
S
Institute of Morphological Sciences, Scientific Campus, University Carlo Bo of Urbino, Urbino, Italy.
Luchetti
F
F
Battistelli
M
M
Della Felice
M
M
Papa
S
S
Piersanti
G
G
Tarzia
G
G
Falcieri
E
E
D017209:Apoptosis; D045744:Cell Line, Tumor; D004247:DNA / Q000737:chemistry; D004587:Electrophoresis, Agar Gel; D004791:Enzyme Inhibitors / Q000494:pharmacology; D004847:Epithelial Cells; D018922:HL-60 Cells; D006801:Humans; D007166:Immunosuppressive Agents / Q000494:pharmacology*; D008854:Microscopy, Electron; D008956:Models, Chemical; D009336:Necrosis; D009369:Neoplasms / Q000188:drug therapy; D065108:Ornithine Decarboxylase Inhibitors; D011073:Polyamines / Q000737:chemistry; D014230:Triazoles / Q000494:pharmacology*
D004791:Enzyme Inhibitors; D007166:Immunosuppressive Agents; D065108:Ornithine Decarboxylase Inhibitors; D011073:Polyamines; D014230:Triazoles; C030266:3-(2-ethylphenyl)-5-(3-methoxyphenyl)-1H-1,2,4-triazole; D004247:DNA