Vinblastine-C4 alkyl maleoyl and amino acid maleoyl derivatives. II. Experimental antitumor activity against leukemias and human tumor xenografts.
The experimental antitumor activity of new vinca analogues was evaluated in mice. Among the derivatives tested, compounds n.8 and 14 demonstrated good activity against the P388 leukemia. These analogues were further investigated in 3 human carcinomas xenografted in nude mice. Compound n.8 compared favourably with vinblastine in the MX1 xenograft. Derivative n.14 showed activity against HepG2 and MX1 xenografts. As expected, derivative n.14 showed no activity against the CX1 tumor. Because of their significant antitumor activity in different models, further development of these compounds in being considered.
S.A. IRE-CELLTARG, Fleurus, Belgium.
M P
MP
Collard
K S
KS
Rao
A
A
Trouet
D000818:Animals; D005260:Female; D006801:Humans; D007941:Leukemia P388 / Q000188:drug therapy; D051379:Mice; D008807:Mice, Inbred BALB C; D009368:Neoplasm Transplantation; D009374:Neoplasms, Experimental / Q000188:drug therapy*; D013329:Structure-Activity Relationship; D014183:Transplantation, Heterologous; D014747:Vinblastine / Q000031:analogs & derivatives* / Q000627:therapeutic use
D014747:Vinblastine