دورية أكاديمية
Design, synthesis, biological evaluation, and docking studies of novel (imidazol-5-yl)pyrimidine-based derivatives as dual BRAF V600E /p38α inhibitors.
| العنوان: | Design, synthesis, biological evaluation, and docking studies of novel (imidazol-5-yl)pyrimidine-based derivatives as dual BRAF V600E /p38α inhibitors. |
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| المؤلفون: | Ali EMH; Center of Biomaterials, Korea Institute of Science & Technology (KIST School), Seoul, Seongbuk-gu, 02792, Republic of Korea; University of Science & Technology (UST), Daejeon, Yuseong-gu, 34113, Republic of Korea; Pharmaceutical Chemistry Department, Faculty of Pharmacy, Modern University for Technology and Information (MTI), Cairo, 12055, Egypt., El-Telbany RFA; Biochemistry Department, Faculty of Pharmacy, Modern University for Technology and Information (MTI), Cairo, 12055, Egypt., Abdel-Maksoud MS; Medicinal & Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre NRC (ID: 60014618)), Dokki, Giza, 12622, Egypt., Ammar UM; Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, 161 Cathedral Street, Glasgow, G4 0NR, Scotland, United Kingdom., Mersal KI; Center of Biomaterials, Korea Institute of Science & Technology (KIST School), Seoul, Seongbuk-gu, 02792, Republic of Korea; University of Science & Technology (UST), Daejeon, Yuseong-gu, 34113, Republic of Korea., Zaraei SO; Center of Biomaterials, Korea Institute of Science & Technology (KIST School), Seoul, Seongbuk-gu, 02792, Republic of Korea; University of Science & Technology (UST), Daejeon, Yuseong-gu, 34113, Republic of Korea., El-Gamal MI; Department of Medicinal Chemistry, College of Pharmacy, University of Sharjah, Sharjah, 27272, United Arab Emirates; Sharjah Institute for Medical Research, University of Sharjah, Sharjah, 27272, United Arab Emirates; Department of Medicinal Chemistry, Faculty of Pharmacy, University of Mansoura, Mansoura, 35516, Egypt., Choi SI; Department of Pharmaceutical Biochemistry, College of Pharmacy, Kyung Hee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul, 130-701, Republic of Korea., Lee KT; Department of Pharmaceutical Biochemistry, College of Pharmacy, Kyung Hee University, 1 Hoegi-dong, Dongdaemun-gu, Seoul, 130-701, Republic of Korea., Kim HK; Department of Nuclear Medicine, Molecular Imaging & Therapeutic Medicine Research Center, Jeonbuk National University Medical School and Hospital, 20 Geonji-ro, Deokjin-gu, Jeonju, 54907, Republic of Korea; Research Institute of Clinical Medicine of Jeonbuk National University-Biomedical Research Institute of Jeonbuk National University Hospital, 20 Geonji-ro, Deokjin-gu, Jeonju, 54907, Republic of Korea., Lee KH; Center of Biomaterials, Korea Institute of Science & Technology (KIST School), Seoul, Seongbuk-gu, 02792, Republic of Korea; KU-KIST Graduate School of Converging Science and Technology, Korea University, Seoul, 02841, Republic of Korea., Oh CH; Center of Biomaterials, Korea Institute of Science & Technology (KIST School), Seoul, Seongbuk-gu, 02792, Republic of Korea; University of Science & Technology (UST), Daejeon, Yuseong-gu, 34113, Republic of Korea. Electronic address: choh@kist.re.kr. |
| المصدر: | European journal of medicinal chemistry [Eur J Med Chem] 2021 Apr 05; Vol. 215, pp. 113277. Date of Electronic Publication: 2021 Feb 07. |
| 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: | Imidazoles/*pharmacology , Mitogen-Activated Protein Kinase 14/*antagonists & inhibitors , Protein Kinase Inhibitors/*pharmacology , Proto-Oncogene Proteins B-raf/*antagonists & inhibitors , Pyrimidines/*pharmacology, Animals ; Catalytic Domain ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Drug Design ; Drug Screening Assays, Antitumor ; Humans ; Imidazoles/chemical synthesis ; Imidazoles/metabolism ; Mice ; Mitogen-Activated Protein Kinase 14/metabolism ; Molecular Docking Simulation ; Molecular Structure ; Mutation ; Protein Binding ; Protein Kinase Inhibitors/chemical synthesis ; Protein Kinase Inhibitors/metabolism ; Proto-Oncogene Proteins B-raf/genetics ; Proto-Oncogene Proteins B-raf/metabolism ; Pyrimidines/chemical synthesis ; Pyrimidines/metabolism ; Structure-Activity Relationship |
| مستخلص: | The synergistic effect of dual inhibition of serine/threonine protein kinases that are involved in the same signalling pathway of the diseases can exert superior biological benefits for treatment of these diseases. In the present work, a new series of (imidazol-5-yl)pyrimidine was designed and synthesized as dual inhibitors of BRAF V600E and p38α kinases which are considered as key regulators in mitogen-activated protein kinase (MAPK) signalling pathway. The target compounds were evaluated for dual kinase inhibitory activity. The tested compounds exhibited nanomolar scale 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 © 2021 Elsevier Masson SAS. All rights reserved.) |
| فهرسة مساهمة: | Keywords: BRAF(V600E); Imidazol-5-ylpyrimidine; MAPK14; Melanoma; Molecular docking; TNF-α |
| المشرفين على المادة: | 0 (Imidazoles) 0 (Protein Kinase Inhibitors) 0 (Pyrimidines) EC 2.7.11.1 (Braf protein, mouse) EC 2.7.11.1 (Proto-Oncogene Proteins B-raf) EC 2.7.11.24 (Mitogen-Activated Protein Kinase 14) |
| تواريخ الأحداث: | Date Created: 20210218 Date Completed: 20210526 Latest Revision: 20210526 |
| رمز التحديث: | 20221213 |
| DOI: | 10.1016/j.ejmech.2021.113277 |
| PMID: | 33601311 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1768-3254 |
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| DOI: | 10.1016/j.ejmech.2021.113277 |