UniversitÈ Laval

Patrick Poyet

Rene C Gaudreault

Claude Gicquaud

The present invention is concerned with novel anticancer agents having potent antineoplastic activity without systemic toxicity and mutagenicity. The novel anticancer agents of the present invention are derivatives of formula I: ##STR1## wherein: A is O or NH; and

Certain carbanate anti-cancer agents

Carriers for pharmacologic agents comprise nanoerythrosomes, which are vesicles prepared by the extrusion of red blood cell ghosts, the average diameter of these vesicles is 0.1 .mu.m; the daunorubicin was covalently linked to nanoerythrosomes and the cytotoxicity of daunorubicin conjugated to nanoerythrosomes was assessed on P388D.sub.1 cell line; the results indicated that the cytotoxicity of conjugated daunorubicin was higher than the free daunorubicin, similar results were observed on CDF.sub.1 mice bearing grafted P388D.sub.1 leukemia tumors; daunorubicin-nanoerythrosome conjugates had a higher antineoplastic activity than the free bioactive agent.

Nanoerythrosome as bioactive agent carrier

The present invention is concerned with novel anticancer agents having potent antineoplastic activity without systemic toxicity and mutagenicity. The novel anticancer agents of the present invention are derivatives of formula I: ##STR1## wherein: A is O or NH; and B is an aryl group selected from the group consisting of phenyl, indane, fluorene, indazole, indole, and pyridine, the aryl group being substituted with at least one substituent selected from the group consisting of hydrogen, C.sub.1-16 alkyl optionally substituted with one or more OH or SH, lower alkoxy, C.sub.3-6 cycloalkyl, lower alkylthio, nitro, cyano, lower alkene, lower alkyne, OH, SH, carboxy lower alkyl, carboxy lower alkyl esters, amino, N-lower alkyl, N,N-dilower alkyl and halogen; or a prodrug thereof, with the provisos that when A is NH and B is phenyl:

Growing community of inventors

Saint-Redempteur, Canada

Patrick Poyet