دورية أكاديمية

Design and synthesis of VEGFR-2 inhibitors based on oleanolic acid moiety.

التفاصيل البيبلوغرافية
العنوان: Design and synthesis of VEGFR-2 inhibitors based on oleanolic acid moiety.
المؤلفون: Song YL; Department of Pharmaceutical Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China., Zhang PB; Department of Pharmaceutical Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China., Tong RJ; Department of Pharmaceutical Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China., Li L; Department of Pharmaceutical Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China., Meng YQ; Department of Pharmaceutical Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China.
المصدر: Journal of Asian natural products research [J Asian Nat Prod Res] 2021 Feb; Vol. 23 (2), pp. 176-188. Date of Electronic Publication: 2019 Dec 31.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: Informa Healthcare Country of Publication: England NLM ID: 100888334 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1477-2213 (Electronic) Linking ISSN: 10286020 NLM ISO Abbreviation: J Asian Nat Prod Res Subsets: MEDLINE
أسماء مطبوعة: Publication: London : Informa Healthcare
Original Publication: [Newark, N.J.?] : Harwood Academic Publishers,
مواضيع طبية MeSH: Oleanolic Acid*/pharmacology, Cell Proliferation ; Drug Design ; Molecular Docking Simulation ; Molecular Structure ; Structure-Activity Relationship ; Vascular Endothelial Growth Factor Receptor-2/metabolism
مستخلص: In this study, twenty-four oleanolic acid (OA) derivatives were rationally designed based on molecule docking studies and their VEGFR-2 inhibitory activities were tested by Homogeneous time-resolved fluorescence (HTRF) method in vitro . All of the synthesized compounds were identified as new compounds, and the structures of these compounds were determined by 1 H-NMR and ESI-MS. In the screening for VEGFR-2 inhibitors, compounds I 6 and I 7 exhibited excellent inhibitory effect. The results indicated that insertion of phenylurea group with a linker at position C-28 of OA can increase the activity against VEGFR-2 significantly. [Formula: see text].
فهرسة مساهمة: Keywords: Oleanolic acid derivative; VEGFR-2 inhibitor; molecular docking
المشرفين على المادة: 6SMK8R7TGJ (Oleanolic Acid)
EC 2.7.10.1 (Vascular Endothelial Growth Factor Receptor-2)
تواريخ الأحداث: Date Created: 20200101 Date Completed: 20210205 Latest Revision: 20210205
رمز التحديث: 20231215
DOI: 10.1080/10286020.2019.1706500
PMID: 31888388
قاعدة البيانات: MEDLINE
الوصف
تدمد:1477-2213
DOI:10.1080/10286020.2019.1706500