Synthesis and cytotoxic evaluation of novel ester-triazole-linked triterpenoid–AZT conjugates |
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| Institution: | 1. Institute of Chemistry, Vietnam Academy of Science and Technology, 18-Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam;2. SynBioC Research Group, Department of Sustainable Organic Chemistry and Technology, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, B-9000 Ghent, Belgium;1. Jiangsu Province Hi-Tech Key Laboratory for Biomedical Research, School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189, PR China;2. Chinese Acad Sci, Northwest Inst Plateau Biol, Qinghai Key Laboratory of Qinghai-Tibet Plateau Biological Resources, Xining 810000, PR China;3. State Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources (Ministry of Education of China), School of Chemistry and Pharmaceutical Sciences of Guangxi Normal University, Guilin 541004, PR China;1. State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, PR China;2. Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, PR China;3. Department of Organic Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, PR China;4. Department of Microbiology, Immunology and Molecular Genetics, University of Kentucky College of Medicine, 800 Rose Street, Lexington, KY 40536, USA;5. College of Pharmacy and Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, Jinan University, Guangzhou 510632, PR China;1. Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Viale delle Scienze, ed. 17, I-90128 Palermo, Italy;2. Centro Grandi Apparecchiature (CGA) – ATeN Center, University of Palermo, via F. Marini 14, 90128 Palermo, Italy;3. Dipartimento di Scienze Agrarie, Alimentari e Forestali (SAAF), Università degli Studi di Palermo, Viale delle Scienze, ed. 4, I-90128 Palermo, Italy |
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| Abstract: | Betulinic acid and analogous naturally occurring triterpenoid acids were transformed into the corresponding propargyl esters and subsequently deployed as substrates for a click chemistry-mediated coupling with azidothymidine (AZT) en route to novel 1,2,3-triazole-tethered triterpenoid–AZT conjugates. Twelve new hybrids were thus prepared and assessed in terms of their cytotoxic activity, revealing an interesting anticancer activity of five triterpenoid–AZT hybrids on KB and Hep-G2 tumor cell lines. |
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| Keywords: | Triterpenoids AZT Hybrids Cytotoxic agents |
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