Studies in sugar chemistry. VII. Glucuronides of podophyllum derivatives.
The antitumor activities of several glucuronide methyl esters of podophyllum derivatives were tested in vitro against two human tumor cell lines and their drug resistant sublines. The most active compound studied was methyl (4'-carbobenzoxy-4'-demethyl-epipodophyllotoxin-D-glucopyranoside)uronat e 19. Compound 19 was as potent in a colon carcinoma model and was twice as potent in a lung carcinoma model as etoposide 6. In vivo, however, in a mouse leukemia P388 model, it had only marginal activity, with a maximum T/C% value of 125 at 37 mg/kg (iv).
Nudelman
A
A
Chemistry Department, Bar-Ilan University, Ramat Gan, Israel.
Ruse
M
M
Gottlieb
H E
HE
Fairchild
C
C
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000494:pharmacology*; D003110:Colonic Neoplasms / Q000188:drug therapy; D004354:Drug Screening Assays, Antitumor; D005965:Glucuronates / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D007941:Leukemia P388 / Q000188:drug therapy; D008175:Lung Neoplasms / Q000188:drug therapy; D051379:Mice; D008810:Mice, Inbred C57BL; D008811:Mice, Inbred DBA; D010946:Plants, Medicinal; D010947:Plants, Toxic; D011035:Podophyllum / Q000737:chemistry*; D014407:Tumor Cells, Cultured
D000972:Antineoplastic Agents, Phytogenic; D005965:Glucuronates