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Synthesis and antitumor activity of daunorubicin conjugates with of 3,4-methylendioxybenzaldehyde
Affiliation:1. A. N. Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, ul. Vavilova 28, Moscow 119991, Russia;2. Institute of Physiologically Active Compounds, Russian Academy of Sciences, 1 Severny pr., Chernogolovka 142432, Russia;1. Department of Chemistry, Susquehanna University, 514 University Avenue, Selinsgrove, PA 17870, USA;2. Bioactive Botanical Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island, Kingston, RI 02881, USA;1. Genentech Inc., 1 DNA Way, South San Francisco, CA 94080, USA;2. Department of Integrated Structural and Computational Biology, The Scripps Research Institute, 130 Scripps Way, Jupiter, FL 33458, USA;3. WuXi AppTec, 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, China;1. Aix Marseille Univ, CNRS, ICR UMR 7273, Equipe Pharmaco-Chimie Radicalaire, Faculté de Pharmacie, 27 Boulevard Jean Moulin, CS30064, 13385, Marseille Cedex 05, France;2. Université de Limoges, UMR Inserm 1094, Neuroépidémiologie Tropicale, Faculté de Pharmacie, 2 rue du Dr Marcland, 87025, Limoges, France;3. Université de Limoges, BISCEm Mass Spectrometry Platform, CBRS, 2 rue du Pr. Descottes, F-87025, Limoges, France;4. Aix Marseille Univ, IHU Méditerranée Infection, UMR VITROME, Tropical Eukaryotic Pathogens, 19-21 Boulevard Jean Moulin, 13005, Marseille, France;5. LCC-CNRS Université de Toulouse, CNRS, UPS, Toulouse, France;6. UMR 152 PHARMA-DEV, Université de Toulouse, IRD, UPS, Toulouse, France;7. AP-HP, Groupe Hospitalier Pitié-Salpêtrière, Service de Parasitologie Mycologie, Paris, France;8. University of Dundee, School of Life Sciences, Division of Biological Chemistry and Drug Discovery, Dow Street, Dundee, DD1 5EH, Scotland, United Kingdom;9. Toxalim (Research Centre in Food Toxicology), Université de Toulouse, INRA, ENVT, INP-Purpan, UPS, Toulouse, France;10. Normandie Univ, UNICAEN, CERMN, 14000, Caen, France;11. Department of Pharmacology, Toxicology and Pharmacovigilance, CHU Limoges, INSERM, UMR 1248, University of Limoges, Limoges, France;12. CIMI-Paris, Sorbonne Université 91 boulevard de l’Hôpital, 75013, Paris, France
Abstract:The design of hybrid (chimeric) molecules containing two different pharmacophores connected via a spacer (linker) is a promising approach to the functionalization of natural compounds and potentially of drug molecules. These are important examples for the use of this approach with anthracycline antibiotics. The use of this methodology may help to eliminate some of the drawbacks of anthracycline drugs, e.g., high cardiotoxicity and MDR development.
Keywords:Anthracycline antibiotics  Daunorubicin  Anticancer activity  Antitumor conjugates
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