دورية أكاديمية
Novel 2-indolinone thiazole hybrids as sunitinib analogues: Design, synthesis, and potent VEGFR-2 inhibition with potential anti-renal cancer activity.
| العنوان: | Novel 2-indolinone thiazole hybrids as sunitinib analogues: Design, synthesis, and potent VEGFR-2 inhibition with potential anti-renal cancer activity. |
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| المؤلفون: | Mahmoud HK; Department of Chemistry, Faculty of Science, Cairo University, Giza, 12613, Egypt., Farghaly TA; Department of Chemistry, Faculty of Science, Cairo University, Giza, 12613, Egypt; Department of Chemistry, Faculty of Applied Science, Umm Al-Qura University, Makkah Almukkarramah, Saudi Arabia. Electronic address: thoraya-f@hotmail.com., Abdulwahab HG; Pharmaceutical Chemistry Department, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt., Al-Qurashi NT; Department of Basic Science, University College in Adam, Umm Al-Qura University, Makkah Almukkarramah, Saudi Arabia., Shaaban MR; Department of Chemistry, Faculty of Science, Cairo University, Giza, 12613, Egypt; Department of Chemistry, Faculty of Applied Science, Umm Al-Qura University, Makkah Almukkarramah, Saudi Arabia. |
| المصدر: | European journal of medicinal chemistry [Eur J Med Chem] 2020 Dec 15; Vol. 208, pp. 112752. Date of Electronic Publication: 2020 Aug 21. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Editions Scientifiques Elsevier Country of Publication: France NLM ID: 0420510 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1768-3254 (Electronic) Linking ISSN: 02235234 NLM ISO Abbreviation: Eur J Med Chem Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Paris : Editions Scientifiques Elsevier Original Publication: Paris, S.E.C.T. [etc.] |
| مواضيع طبية MeSH: | Antineoplastic Agents/*pharmacology , Kidney Neoplasms/*drug therapy , Oxindoles/*pharmacology , Protein Kinase Inhibitors/*pharmacology , Thiazoles/*pharmacology , Vascular Endothelial Growth Factor Receptor-2/*antagonists & inhibitors, Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/metabolism ; Binding Sites ; Cell Line, Tumor ; Drug Screening Assays, Antitumor ; Humans ; Molecular Docking Simulation ; Oxindoles/chemical synthesis ; Oxindoles/metabolism ; Protein Binding ; Protein Kinase Inhibitors/chemical synthesis ; Protein Kinase Inhibitors/metabolism ; Sunitinib/chemistry ; Thiazoles/chemical synthesis ; Thiazoles/metabolism ; Vascular Endothelial Growth Factor Receptor-2/chemistry ; Vascular Endothelial Growth Factor Receptor-2/metabolism |
| مستخلص: | Novel 2-indolinone thiazole hybrids were designed and synthesized as VEGFR-2 inhibitors based on sunitinib, an FDA-approved anticancer drug. The proposed structures of the prepared 2-indolinone thiazole hybrids were confirmed based on their spectral data and CHN analyses. The target compounds were screened in vitro for their anti-VEGFR-2 activity. All tested compounds exhibited a potent submicromolar inhibition of VEGFR-2 kinase with IC Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. (Copyright © 2020 Elsevier Masson SAS. All rights reserved.) |
| فهرسة مساهمة: | Keywords: Anti-renal cancer activity; Docking study; Indolinone; Sunitinib; Thiazoles |
| المشرفين على المادة: | 0 (Antineoplastic Agents) 0 (Oxindoles) 0 (Protein Kinase Inhibitors) 0 (Thiazoles) EC 2.7.10.1 (KDR protein, human) EC 2.7.10.1 (Vascular Endothelial Growth Factor Receptor-2) V99T50803M (Sunitinib) |
| تواريخ الأحداث: | Date Created: 20200918 Date Completed: 20210526 Latest Revision: 20210526 |
| رمز التحديث: | 20231215 |
| DOI: | 10.1016/j.ejmech.2020.112752 |
| PMID: | 32947227 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1768-3254 |
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| DOI: | 10.1016/j.ejmech.2020.112752 |