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P-43 ISBOMC `10 5.7 – 9.7. 2010 Ruhr-Universität Bochum Bengin Reactions with Acetylferrocene for the Synthesis of some Ferrocenylhydrazones of Expected Biological Activity Mohamed A. Metwally *a a Chemistry Department, Faculty of Science, University of Mansoura, P.O. Box 23, Mansoura, Egypt. Email: mamegs@mans.edu.eg Waste-free environmentally benign solid-state reactions means 100% yield of one product without any necessity for purifying workup by recrystallization, chromatography, etc. Continuing our earlier studies on ferrocenes, 1,2 the solid state reaction of acetylferrocene using the ball-milling technique with several hydrazines and hydrazides resulted in the formation of the hydrazones 1 in quantitative yields (95-98%). The products were screened for their antibacterial and antifungal activities and gave promising results. References Fe 1. M.A. Metwally, E.E.M. Kandel, F.A. Amer, J. Indian Chem. Soc. 1987, 64, 517-518. 2. M.A. Metwally, F.A. Amer, J. Indian Chem. Soc. 1988, 65, 51-53. CH 3 C 101 N.NH.R 1, a, R= -C 6H 5NO 2-p, b, R= -C 6H 3(NO 2) 2-2,4-, c, R= -SO 2C 6H 5, d, R= -CSNH 2, e, R= -COCH 2CN
P-44 ISBOMC `10 5.7 – 9.7. 2010 Ruhr-Universität Bochum Ferrocenyl Flavonoids: A Novel Class of Cytotoxics Jean-Philippe Monserrat, a Elizabeth A. Hillard, a and Gérard Jaouen *a a Organometallic Medicinal Chemistry Team, UMR 7223, Laboratoire Charles Friedel 11, rue Pierre et Marie Curie 75231 Paris Cedex 05 Occupying the second step of the mortality podium in the western countries, cancer has become one of the most widely studied diseases in the world, and one of the most challenging targets for scientists. In order to combat the common problem of drug resistance, we have decided to approach the problem via the redox machinery of the cell. It is now accepted that elevated levels of cellular oxidative stress and dependence on ROS-signaling for mitosis and apoptosis represent a specific vulnerability of cancer cells that can be targeted by redox modulators. 1 Ferrocene is an organometallic complex that possesses a stable and reversible redox couple, and possesses many attractive qualities for use in medicinal chemistry. Ferrocene-tamoxifen derivatives, in particular, are known to be highly toxic against cancer cells via a redox mechanism. 2 Fe O OH hydroxyferrocifen N 102 O OH O quercetin Flavonoids are a large class of natural products, some of which are active against cancer and are thought to act, at least partially, via a redox mechanism. For instance, quercetin, in the process of scavenging free radicals, can be converted to four quinone forms (QQ), which can form adducts with glutathione, thus disturbing the redox balance of the cell. 3 Other polyphenols specifically act as prooxidants in oxidizing environments. 4 Because some cancer cells are under oxidative stress, these properties could be useful in the design of selective cancer agents. 5,6 By the introduction of ferrocene, we hope to modulate the flavonoids’ redox properties and enhance their antiproliferative effects. We have recently discovered a novel reaction which gives easy access to the first reported ferrocenyl flavones. Preliminary results show that the antiproliferative effects of ferrocene flavones against the highly aggressive B16 mouse melanoma cell line are considerably stronger than those of organic flavones, with IC50 values in the low micromolar range. The synthesis and biological results of this original class of molecules will be presented. References 1. G. T. Wondrak, Antiox. Redox. Sign. 2009, 11, 3013-3069. 2. E. A. Hillard, A. Vessières, L. Thouin, G. Jaouen and C. Amatore, Angew. Chem. Int. Ed. 2006, 45, 285-290. 3. W. Boots, H. Li, R. P. F. Schins, R. Duffin, J. W. M. Heemskerk, A. Bast and G. R. M. M. Haenen, Toxicol. App.Pharmacol. 2007, 222, 89-96. 4. Simić, D. Manojlović, D. Šegan and M. Todorović, Molecules, 2007, 12, 2327. 5. H. Pelicano, D. Carney and P. Huang, Drug Resist. Update 2004, 7, 97-110. 6. Hoffman, L. M. Spetner and M. Burke, J. Theor. Biol. 2001, 211, 403-407. HO OH OH OH
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Obiora Augustine Orakwue Hyqid Nige
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