Synthesis and antitumour activity of 4-hydroxy-2-pyridone derivatives

4-hydroxy-2-pyridone derivatives 2 were prepared by reaction of 3-amino-3-d ialkylaminopropenoates with bis(2,4,6-trichlorophenyl)malonate. These compo unds were further reacted with a set of aldehydes to give bis(pyridyl)metha nes 3 and 4. The newly synthesized compounds 2, 3 and 4 were evaluated in v itro as antitumour agents against 60 human tumour cell lines. Some derivati ves exhibit tumour growth inhibition activity. In particular, derivative 4g , the most active of the series, possesses significant activity on all cell lines at concentrations ranging from 1 x 10(-6) to 1 x 10(-5) M. (C) 2000 Editions scientifiques et medicales Elsevier SAS.