Synthesis and antibacterial activity of a number of 7-O-epoxyalkyl derivatives of daunomycinone prepared from 7-O-alkenyl derivatives of daunomycinone are described along with their inhibitory effect on leukemia P 388 cells.
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Complex associations between cancer progression and immune gene expression reveals early influence of transmissible cancer on Tasmanian devils.
Front Immunol
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Deakin University, School of Life and Environmental Sciences, Centre for Integrative Ecology, Geelong, VIC, Australia.
The world's largest extant carnivorous marsupial, the Tasmanian devil, is challenged by Devil Facial Tumor Disease (DFTD), a fatal, clonally transmitted cancer. In two decades, DFTD has spread across 95% of the species distributional range. A previous study has shown that factors such as season, geographic location, and infection with DFTD can impact the expression of immune genes in Tasmanian devils.
View Article and Find Full Text PDFIntergenomic signatures of coevolution between Tasmanian devils and an infectious cancer.
Proc Natl Acad Sci U S A
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Department of Integrative Biology, University of South Florida, Tampa, FL 33620.
Coevolution is common and frequently governs host-pathogen interaction outcomes. Phenotypes underlying these interactions often manifest as the combined products of the genomes of interacting species, yet traditional quantitative trait mapping approaches ignore these intergenomic interactions. Devil facial tumor disease (DFTD), an infectious cancer afflicting Tasmanian devils (), has decimated devil populations due to universal host susceptibility and a fatality rate approaching 100%.
View Article and Find Full Text PDFInhibitory activity of four demethoxy fluorinated anthracycline analogs against five human-tumor cell lines.
Bioorg Med Chem Lett
November 2010
Department of Chemistry, American University, 4400 Massachusetts Avenue, NW, Washington, DC 20016, USA.
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.
View Article and Find Full Text PDFAnthracycline glycosides of 2,6-dideoxy-2-fluoro-alpha-L-talopyranose.
Carbohydr Res
November 2006
Department of Chemistry, American University, 4400 Massachusetts Avenue, NW, Washington, DC 20016, USA.
The methyl beta-glycoside of the title sugar, obtained from 2-deoxy-2-fluoro-beta-D-glucopyranose tetraacetate by a sequence with detailed characterization of all intermediates, was converted by acetolysis-bromination into 3,4-di-O-acetyl-2,6-dideoxy-2-fluoro-alpha-L-talopyranosyl bromide, coupling of which with (7S,9S)-4-demethoxydaunomycinone afforded the 3,4-diacetate of 4-demethoxy-9-O-(2,6-dideoxy-2-fluoro-alpha-L-talopyranosyl)daunomycinone (19). The antitumor-active 19 was converted by way of its 14-bromo derivative into the 14-hydroxy analogue, the antitumor-active 4-demethoxyadriamycinone glycoside 21.
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Bioorg Med Chem Lett
December 2002
Division of Pharmacognosy, Department of Pharmacy, University of Athens, Panepistimiopolis-Zografou, Greece.
The preparation and cytotoxic activity of 4'-azido-3'-bromo-3'-deamino-4'-deoxydaunorubicin is described. The new compound was found to be less active in vitro than adriamycin against L1210 and the sensitive cell lines KB-3-1 and MES-SA, but retained interesting cytotoxicity against the adriamycin resistant subline KB-A1 and the multidrug resistant MES-SA/Dx5 subline.
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