New .alpha.-amino phosphonic acid derivatives of vinblastine: chemistry and antitumor activity
作者:Gilbert Lavielle、Patrick Hautefaye、Corinne Schaeffer、Jean A. Boutin、Claude A. Cudennec、Alain Pierre
DOI:10.1021/jm00111a012
日期:1991.7
A series of new amino phosphonicacid derivatives of vinblastine (1, VLB) has been synthesized and tested in vitro and in vivo for antitumor activity. The compounds were obtained from O4-deacetyl-VLB azide. All of the new products studied were capable of inhibiting tubulin polymerization in vitro. The most potent antitumor compounds bore an alkyl substituent on the phosphonate. In these compounds,
The invention is related to phosphorus substituted anti-viral inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.