Synthesis and antitumour activity of 4-hydroxy-2-pyridone derivatives.
M T Cocco, C Congiu, V Onnis
Index: Eur. J. Med. Chem. 35(5) , 545-52, (2000)
Full Text: HTML
Abstract
4-hydroxy-2-pyridone derivatives 2 were prepared by reaction of 3-amino-3-dialkylaminopropenoates with bis(2,4, 6-trichlorophenyl)malonate. These compounds were further reacted with a set of aldehydes to give bis(pyridyl)methanes 3 and 4. The newly synthesized compounds 2, 3 and 4 were evaluated in vitro as antitumour agents against 60 human tumour cell lines. Some derivatives 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.
Related Compounds
Related Articles:
Synthesis of diazaphenoxathiin nucleosides from 3-deazauridine and their chemical properties.
1983-01-01
[Nucleic Acids Symp. Ser. (12) , 13-6, (1983)]
Structure-activity relationship of ligands of dihydrouracil dehydrogenase from mouse liver.
1989-05-01
[Biochem. Pharmacol. 38(9) , 1471-80, (1989)]
[Presynaptic effects of aminopyridines on the neuromuscular junction of vertebrates].
1985-01-01
[J. Pharmacol. 16 Suppl 2 , 109-44, (1985)]
1983-01-01
[Ther. Drug Monit. 5(4) , 491-6, (1983)]
New bis(pyridyl)methane derivatives from 4-hydroxy-2-pyridones: synthesis and antitumoral activity
2003-01-01
[Eur. J. Med. Chem. 38(1) , 37-47, (2003)]