Identification of novel bivalent mimetics of annonaceous acetogenins via a scaffold-hopping strategy |
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| Institution: | 1. Laboratory of Medicinal Chemistry, Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou 510530, China;2. Division of Molecular Carcinogenesis and Targeted Therapy for Cancer, State Key Laboratory of Biomembrane and Membrane Biotechnology, Institute of Zoology, Chinese Academy of Sciences, Beijing 100101, China;3. Department of Translational Imaging, The Houston Methodist Research Institute, Houston, TX 77030, United States;4. State Key Laboratory of Coordination Chemistry, Nanjing National Laboratory of Microstructures, School of Chemistry and Chemical Engineering, Nanjing University, 22 Hankou Road, Nanjing 210093, China;1. CNRS, SRSMC, UMR 7565, Vandœuvre-lès-Nancy, F-54506, France;2. Université de Lorraine, SRSMC, UMR 7565, Nancy F-54001, France;3. ABC Platform®, Nancy F-54001, France;1. Faculty of Science, Beirut Arab University, P.O. Box 11-5020 Riad El Solh, Beirut 1107 2809, Lebanon;2. Khalifa University, P.O. Box 57, Abu Dahbi, United Arab Emirates;1. Dipartimento di Farmacia-Scienze del Farmaco, Università degli Studi ‘Aldo Moro’ di Bari, Via Orabona 4, 70126 Bari, Italy;2. Università degli Studi di Firenze, Dipartimento di Chimica, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy;3. Università degli Studi di Firenze, Neurofarba Dept., Section of Pharmaceutical and Nutriceutical Sciences, Via U. Schiff 6, 50019 Sesto Fiorentino (Firenze), Italy;1. Department of Otolaryngology, The First People''s Hospital of Foshan, Foshan 528000, PR China;2. Department of Otolaryngology, Sun Yat-Sen Memorial Hospital and Institute of Hearing and Speech-Language Science, Sun Yat-Sen University, Guangzhou 510120, PR China |
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| Abstract: | A series of novel bivalent mimetics of annonaceous acetogenins have been designed, synthesized, and evaluated. Among these, compound 7 bearing a homopiperazine ring in the middle region exhibited more potent growth inhibitory activity and higher selectivity against cancer cells over normal cells by comparison with AA005. This work indicates that modification of the middle piperazine ring is a useful optimizing tool for the simplified acetogenin mimetics. |
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| Keywords: | Annonaceous acetogenins Homopiperazine Bivalent analogues Cytotoxicity Selectivity |
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