Inhibitory activity of four demethoxy fluorinated anthracycline analogs against five human-tumor cell lines |
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Authors: | Derek Horton Anakshi Khare |
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Affiliation: | 1. Department of Chemistry, American University, 4400 Massachusetts Avenue, NW, Washington, DC 20016, USA;2. Department of Chemistry, Lucknow University, Lucknow 226007, India |
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Abstract: | 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. |
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