Syntheses of novel antitumor dihydroxanthone derivatives with inhibitory activity against DNA topoisomerase II.
A series of methoxycarbonyl group modified nidulalin A analogs were synthesized to improve stability against esterases. The amide derivatives showed cytotoxic activity along with inhibitory activity against DNA topoisomerase II. Among the analogs, amide 9a exhibited antitumor activity in Colon 26 murine tumor model.
Sato
S
S
Pharmaceutical Research Laboratories, Ajinomoto Co., Inc., Kawasaki, Japan.
Suga
Y
Y
Yoshimura
T
T
Nakagawa
R
R
Tsuji
T
T
Umemura
K
K
Andoh
T
T
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D059005:Topoisomerase II Inhibitors; D014407:Tumor Cells, Cultured; D014970:Xanthines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D059005:Topoisomerase II Inhibitors; D014970:Xanthines