Efficient synthesis of eudistomin U and evaluation of its cytotoxicity |
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| Affiliation: | 1. School of Chemical Sciences, University of Auckland, Private Bag 92019, Auckland, New Zealand;2. Laboratoire Molécules de Communication et Adaptation des Micro-organismes, UMR 7245 CNRS, Muséum National d''Histoire Naturelle, 57 rue Cuvier, 75005 Paris, France;1. Academy of Scientific and Innovative Research (AcSIR), New Delhi 110025, India;2. Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India;3. Centre for Cellular and Molecular Biology, Hyderabad 500007, India;4. National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500 037, India;5. School of Pharmaceutical Education and Research, Jamia Hamdard University, New Delhi 110062, India;1. Department of Chemistry and Centre of Advanced Studies in Chemistry, Panjab University, Chandigarh 160 014, India;2. Department of Microbial Biotechnology, Panjab University, Chandigarh 160 014, India;3. National Interdisciplinary Centre of Vaccine, Immunotherapeutics and Antimicrobials (NICOVIA), Panjab University, Chandigarh 160 014, India;1. Department of Pharmaceutical Chemistry, International Medical University, No. 126, Jalan Jalil Perkasa 19, Bukit Jalil 57000, Kuala Lumpur, Malaysia;2. Centre for Drug Research, Universiti Sains Malaysia, Minden 11800, USM, Penang, Malaysia |
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| Abstract: | Eudistomin U is a member of a subclass of naturally occurring indole alkaloids known as β-carbolines. These molecules are reported to have diverse biological activity and high binding affinity to DNA, which make them attractive targets for total synthesis. We describe an efficient, five-step synthesis of eudistomin U by employing two key reactions: a Bischler–Napieralski cyclization and a Suzuki cross coupling. We also describe the cytotoxicity of eudistomin U against various cancer cell lines and human pathogens, in which we observed potent antibacterial activity against Gram-positive bacteria. |
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| Keywords: | β-Carboline Suzuki cross coupling Eudistomin U Antibacterial Palladium catalysis |
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