Optimised synthesis of diamino-triazinylmethyl benzoates as inhibitors of Rad6B ubiquitin conjugating enzyme |
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| Affiliation: | 1. School of Pharmacy and Pharmaceutical Sciences, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff CF10 3NB, Wales, UK;2. Faculty of Pharmacy, Zagazig University, Zagazig, Egypt;3. Karmanos Cancer Institute, Wayne State University School of Medicine, Department of Oncology, 110 E. Warren Avenue, Detroit, MI 48201, USA;1. School of Safety Science and Engineering, Henan Polytechnic University, Jiaozuo Henan 454000, PR China;2. National Engineering Research Center for Coal & Gas Control, China University of Mining & Technology, Xuzhou Jiangsu 221116, PR China;3. Haizi Coal Mine of of Huaibei Mining Corporation Limited, Huaibei, Anhui 235000, China;1. Department of Chemistry, State University of New York at Buffalo, Buffalo, NY 14260, USA;2. Laboratory of Molecular Modeling and Drug Design, Lindsley F. Kimball Research Institute of the New York Blood Center, 310 E 67th Street, New York, NY 10065, USA;1. Department of Chemistry, Jamia Millia Islamia (Central University), New Delhi 110025, India;2. Dr. B. R. Ambedkar Centre for Biomedical Research, University of Delhi, New Delhi 110007, India;3. Department of Chemistry, B. R. Ambedkar Bihar University, Muzaffarpur 842001, Bihar, India;4. Department of Chemistry, Indian Institute of Technology Delhi, Hauz Khas, New Delhi 110016, India;5. Kusuma School of Biological Sciences, IIT Delhi, New Delhi 110016, India;6. Supercomputing Facility for Bioinformatics & Computational Biology, IIT Delhi, New Delhi 110016, India;1. Organic Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Assiut Branch, 71524 Assuit, Egypt;2. Medicinal Department, Faculty of Pharmacy, Minia University, 61519 El Minia, Egypt;3. Organic and Medicinal Chemistry Department, Faculty of Pharmacy, University of Sadat City, 32958 Menoufia, Egypt;4. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt;5. Chemistry Department, Florida Institute of Technology, Melbourne, FL 32901, USA;6. Chemistry Department, Faculty of Science, Minia University, 61519 El-Minia, Egypt |
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| Abstract: | Recently, we have identified the first inhibitors of Rad6B, an E2 enzyme essential for post-replication DNA repair and a potential new drug target for the treatment of breast cancer. We report two newly optimised synthetic routes to our [4-amino-6-(phenylamino)-1,3,5-triazin-2-yl]methyl 4-nitrobenzoate target compounds TZ8 and TZ9 with general applicability for further structure–activity relationship studies around this pharmacophore. The key step involved the condensation/cyclisation between phenylbiguanide and either ethyl bromoacetate or dimethyloxalate in good yield. |
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| Keywords: | Triazines Biguanides Rad6B inhibitors Antitumour agents |
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