دورية أكاديمية

Synthesis, antiviral and cytotoxic activity of novel terpenyl hybrid molecules prepared by click chemistry

التفاصيل البيبلوغرافية
العنوان: Synthesis, antiviral and cytotoxic activity of novel terpenyl hybrid molecules prepared by click chemistry
المؤلفون: Pertino, M.W., Petrera, E., Edith Alché, L., Schmeda-Hirschmann, G.
المجموعة: Biblioteca Digital FCEN-UBA (Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires)
مصطلحات موضوعية: Antiviral, Click chemistry, Cytotoxicity, Hybrid molecules, Terpenes, antineoplastic agent, antivirus agent, terpene, animal, carbon nuclear magnetic resonance, chemistry, drug effect, drug screening, electrospray mass spectrometry, human, Human alphaherpesvirus 1, mouse, preclinical study, proton nuclear magnetic resonance, RAW 264.7 cell line, synthesis, tumor cell line, Animals, Antineoplastic Agents, Antiviral Agents, Carbon-13 Magnetic Resonance Spectroscopy, Cell Line, Tumor, Drug Evaluation, Preclinical
الوصف: Naturally occurring terpenes were combined by click reactions to generate sixteen hybrid molecules. The diterpene imbricatolic acid (IA) containing an azide group was used as starting compound for the synthesis of all the derivatives. The alkyne group in the terpenes cyperenoic acid, dehydroabietinol, carnosic acid γ-lactone, ferruginol, oleanolic acid and aleuritolic acid was obtained by esterification using appropriate alcohols or acids. The hybrid compounds were prepared by combining the IA azide function with the different terpene-alkynes under click chemistry conditions. The cytotoxic activity of the terpene hybrids 1–16 was assessed against Vero cells and tumour cell lines (HEP-2, C6 and Raw 264.7). Compounds 1, 2, 3 and 7 showed cytotoxic activity against the tested cell lines. The antiviral activity of the compounds was evaluated against HSV-1 KOS, Field and B2006 strain. For the pairs of hybrid compounds formed between IA-diterpene (compounds 3–8, except for compound 7), a moderate activity was observed against the three HSV-1 strains with an interesting selectivity index (SI ≥10, SI = CC50/CE50) for some compounds. © 2018 by the authors.
نوع الوثيقة: journal/newspaper
اللغة: unknown
العلاقة: http://hdl.handle.net/20.500.12110/paper_14203049_v23_n6_p_PertinoTest
الإتاحة: https://doi.org/20.500.12110/paper_14203049_v23_n6_p_PertinoTest
https://hdl.handle.net/20.500.12110/paper_14203049_v23_n6_p_PertinoTest
حقوق: info:eu-repo/semantics/openAccess ; http://creativecommons.org/licenses/by/2.5/arTest
رقم الانضمام: edsbas.3272566E
قاعدة البيانات: BASE