Inhibitory effect of new imidazole derivatives on the proliferation and nucleic acid synthesis of leukemic cells.
New derivatives of imidazothiazole and imidazobenzothiazole were tested in vitro for their potential antiproliferative activity. Four imidazobenzothiazole derivatives exhibited a cytotoxic activity against two leukemic cell lines, compound I being the most effective. Cell cycle kinetics studies showed that this drug delays the progression of cells from G1 to S and G2 M phases. An inhibitory effect on DNA and RNA synthesis was also observed. The antiproliferative effect of this compound, analogue of immunosuppressive agents, suggested that it could be of interest for a therapeutic use and for the synthesis of new derivatives.
Nafziger
J
J
Laboratoire d'Hématologie, Faculté des Sciences Pharmaceutiques et Biologiques, Paris, France.
Guillosson
J J
JJ
Adam
Y
Y
Hecquet
C
C
Payard
M
M
Loiseau
M
M
D002453:Cell Cycle / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects; D002942:Circular Dichroism; D004247:DNA / Q000096:biosynthesis / Q000187:drug effects* / Q000378:metabolism; D004996:Ethidium / Q000378:metabolism; D006801:Humans; D007093:Imidazoles / Q000494:pharmacology*; D007700:Kinetics; D012313:RNA / Q000096:biosynthesis / Q000187:drug effects* / Q000378:metabolism; D014407:Tumor Cells, Cultured
D007093:Imidazoles; D012313:RNA; D004247:DNA; D004996:Ethidium