Synthesis of antineoplaston A10 analogs as potential antitumor agents
Several aniline mustard analogues were obtained by introducingN,N-bis(2-chloroethyl)amino moiety to phenyl ring of A10 analogues in order to increase reactivity of A10 analogs and selectivity into DNA. Thein vitro antitumor activity of synthesized compounds was evaluated using five different solid tumor cell lines by SRB method. Aniline mustard analogues exhibited more potent antitumor activity than A10 analogs. Especially,m-aniline mustard of benzoyl analogue displayed remarkable antitumor activity.
Key wordsAntineoplaston A10 Aniline mustards Piperidinedione derivatives Antitumor agent
Unable to display preview. Download preview PDF.
- Burzynski, S. R. and Georgiades, J., Effect of urinary peptides on DNA, RNA and protein synthesis in normal and neoplastic cells.Bed. Proc., 32, 766 (1973).Google Scholar
- Burzynski, S. R., Mohabbat, M. O. and Burzynski, B., Toxicology studies of oral formation of antineoplaston A10 in cancer patients.Drug Exp. Clin. Res., 10, 611–619 (1984).Google Scholar
- Burzynski, S. R., Synthetic antineoplastons and analogs.Drugs of the future, 11, 679 (1986).Google Scholar
- Burzynski, S. R. and Kubove, E., Toxicology studies of antineoplaston A10 injections.2nd Bien. Conf. Ind. Soc. Onc., Bombay, Feb 9–14 (1986).Google Scholar
- Burzynski, S. R., Urine peptide for the treatment of Parkinson's disease. PCT Int. App. WO9204, 143 (1992).Google Scholar
- De, A.U. and Pal, D., Possible antineoplastic agents I.J. Pharm. Sci., 64, 263 (1975).Google Scholar
- Hendry, L. B., Muldon, T. G., Burzynski, S. R., Copland, J. A. and Lehner, A. F., Stereochemical modelling studies of the interaction of antineoplaston A10 with DNA.Drugs Expl. Clin. Res., 13, 77 (1987).Google Scholar
- Hendry, L. B., Chu, C. K., and Mahesh, V. B., WO91/16309, (1991).Google Scholar
- Niculescu-Duvaz, I., Feyns, V., Salvaniu, M., Ionescu, M., Serban, A. and Cambanis, A., Potential antitumor agents VI. New aromatic nitrogen mustards with good antitumor activity.Bevue Roumaine de Chimie, 14, 535 (1969).Google Scholar