By Waldemar Priebe
content material: Unresolved structure-activity relationships in anthracycline analogue improvement / Edward M. Acton --
Non-cross-resistant anthracyclines with diminished basicity and elevated balance of the glycosidic bond / Waldemar Priebe, Piotr Skibicki, Oscar Varela, Nouri Neamati, Marcos Sznaidman, Krzysztof Dziewiszek, Grzegorz Grynkiewicz, Derek Horton, Yiyu Zou, Yi-He Ling, and Roman Perez-Soler --
Fluorinated anthracyclinones and their glycosylated items / Antonio Guidi, Franca Canfarini, Alessandro Giolitti, Franco Pasqui, Vittorio Pestellini, and Federico Arcamone --
Semisynthetic rhodomycins and anthracycline prodrugs / Cenek Kolar, Klaus Bosslet, Jörg Czech, Manfred Gerken, Peter Hermentin, Dieter Hoffmann, and Hans-Harold Sedlacek --
artificial concepts for reversal of anthracycline resistance and cardiotoxicity / Claude Monneret, Jean-Claude Florent, Jean-Pierre Gesson, Jean-Claude Jacquesy, François Tillequin, and Michel Koch --
Synthesis and organic actions of fluorinated daunorubicin and doxorubicin analogues / Tsutomu Tsuchiya and Yasushi Takagi --
Redox chemistry of anthracyclines and use of oxomorpholinyl radicals / Tad H. Koch and Giorgio Gaudiano --
Synthesis of anthraquinone analogues of associated anthracycline / Ping Ge and Richard A. Russell --
Synthesis and research of structure-activity relationships of recent periods of anthracyclines / Antonino Suarato, Francesco Angelucci, Alberto Bargiotti, Michele Caruso, Daniela Faiardi, Laura Capolongo, Cristina Geroni, Marina Ripamonti, and Maria Grandi --
Molecular attractiveness of DNA through daunorubicin / Jonathan B. Chaires --
Adducts of DNA and anthracycline antibiotics : constructions, interactions, and actions / Jasmine Y.-T. Wang, Mark Chao, and Andrew H.-J. Wang --
DNA topoisomerases and their inhibition via anthracyclines / Yves Pommier --
Anthracycline antihelicase motion : new mechanism with implications for guanosine-cytidine intercalation specificity / Nicholas R. Bachur, Robin Johnson, Fang Yu, Robert Hickey, and Linda Malkas --
Membrane biophysical parameters influencing anthracycline motion / Ratna Mehta and Thomas G. Burke --
sign transduction platforms in doxorubicin hydrochloride mechanism of motion / Paul Vichi, James music, Jean Hess, and Thomas R. Tritton --
research of multidrug transporter in dwelling cells : program to uptake and liberate of anthracycline derivatives by way of drug-resistant K562 cells / Arlette Garnier-Suillerot, Frédéric Frézard, Marie-Nicole Borrel, Elene Pereira, Jolanta Tarasiuk, and Marina Fiallo --
position of reactive-oxygen metabolism in cardiac toxicity of anthracycline antibiotics / James H. Doroshow --
Amelioration of anthracycline-induced cardiotoxicity by means of natural chemical compounds / Donald T. Witiak and Eugene H. Herman --
Use of drug companies to ameliorate the healing index of anthracycline antibiotics / Roman Perez-Soler, Steven Sugarman, Yiyu Zou, and Waldemar Priebe.
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Extra resources for Anthracycline Antibiotics. New Analogues, Methods of Delivery, and Mechanisms of Action
1 mg caused lesions in all ten animals tested (53). 2'-Iodo-3'-deamino Anthracyclines Demethoxylated at the Aglycon at C-4. It was clear to us that any aglycon selected from aglycons previously shown to form active drug in combination with natural sugar should also give active drug when connected through a glycosidic bond with 2'-halo sugars in the amanno or a-talo configuration. Interesting biological properties of idarubicin (4-demethoxydaunorubicin) and its increased potency led to the selection of 4-demethoxydaunomycinone to study synergistic effects of the aglycon and the 2'-halo sugar.
Priebe, W. S. Patent. 1985, 4,537,882, August 27. ; Priebe, W. Carbohydr. Res. 1985, 136, 391. ; Varela, O. Carbohydr. Res. 1985, 144, 305. ; Ok, K. ; Wako, N . ; Umezawa, H . J. Antibiot. 1986, 39, 731. Ok, K. ; Umezawa, H . Carbohydr. Res. 1987, 169, 69. ; Chisato, N . ; Yoneta, T. J. Antibiot. 1988, 41, 988. ; Hermentin, P. J. Carbohydr. Chem. 1989, 8, 247. Florent, J. ; Monneret, C. J. Antibiot. 1989, 22, 1823. ; ACS Symposium Series; American Chemical Society: Washington, DC, 1994. 46 51.
48 ANTHRACYCLINE ANTIBIOTICS activity in important tumor types) severely limit its clinical use. Since the discovery of doxorubicin, the chemists have probably synthesized more than 2000 analogues, in order to enlarge the spectrum of antitumor activity and to overcome the pharmaceutical and toxicological limitations (4). " witnesses the scepticism that is starting to pervade the relevant scientific quarters with respect to the likelihood of further progress in this specific area. Here, an account of the synthesis of anthracycline analogues carrying one or more fluorine atoms on the aglycone moiety will be given.