Synthesis and antitumor activity of quaternary salts of 2-(2'-oxoalkoxy)-9-hydroxyellipticines.
Various kinds of water-soluble quaternary salts of 2-(2'-oxoalkoxy)-9-hydroxyellipticines were synthesized in a search for compounds with potent antitumor activity and low toxicity. Some compounds exhibited more potent antitumor activities than elliptinium (1) and SUN 4599 (3). In particular, 2-(3'-methoxy-2'-oxopropanoxy)-9- hydroxy-5,11-dimethyl-6H-pyrido[4,3-b]carbazolium bromide (4d) showed potent antitumor activities against P388 leukemia, colon 26, and Lewis lung carcinoma.
Harada
N
N
Lead Optimization Research Laboratory, Tanabe Seiyaku Co., Ltd., Saitama, Japan.
Kawaguchi
T
T
Inoue
I
I
Ohashi
M
M
Oda
K
K
Hashiyama
T
T
Tsujihara
K
K
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology*; D018827:Carcinoma, Lewis Lung / Q000188:drug therapy; D003110:Colonic Neoplasms / Q000188:drug therapy; D004354:Drug Screening Assays, Antitumor; D004611:Ellipticines / Q000737:chemistry* / Q000494:pharmacology*; D007941:Leukemia P388 / Q000188:drug therapy; D008297:Male; D051379:Mice; D051381:Rats
D000970:Antineoplastic Agents; D004611:Ellipticines