Inhibitory activity of four demethoxy fluorinated anthracycline analogs against five human-tumor cell lines.
Four anthracycline analogs synthesized in our laboratory were evaluated in comparison with adriamycin (doxorubicin) for their growth-inhibitory effect against five human-tumor cell lines, including lung carcinoma, colon adenocarcinoma, breast adenocarcinoma, melanoma, and glioblastoma. The compounds included 4-demethoxy-7-O-(2,6-dideoxy-2-fluoro--l-talopyranosyl)daunomycinone (2), its 3',4'-diacetate (1), its 14-bromo derivative 3, and its 14-hydroxy analog, namely 4-demethoxy-7-O-(2,6-dideoxy-2-fluoro-α-l-talopyranosyl)adriamycinone (4). Compounds 1, 2, and 3 showed moderate cytotoxic effect in most of the cell lines, while compound 4 had a strong effect, comparable to or better than that of adriamycin in most of the cell lines.
Horton
Derek
D
Department of Chemistry, American University, 4400 Massachusetts Avenue, NW, Washington, DC 20016, USA. carbchm@american.edu
Khare
Anakshi
A
D018943:Anthracyclines / Q000138:chemical synthesis* / Q000494:pharmacology*; D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004247:DNA / Q000378:metabolism; D003630:Daunorubicin / Q000031:analogs & derivatives / Q000494:pharmacology; D004317:Doxorubicin / Q000031:analogs & derivatives / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans
D018943:Anthracyclines; D000903:Antibiotics, Antineoplastic; D004317:Doxorubicin; D004247:DNA; D003630:Daunorubicin