دورية أكاديمية
Structural optimization of 4-(imidazol-5-yl)pyridine derivatives affords broad-spectrum anticancer agents with selective B-RAF V600E /p38α kinase inhibitory activity: Synthesis, in vitro assays and in silico study.
| العنوان: | Structural optimization of 4-(imidazol-5-yl)pyridine derivatives affords broad-spectrum anticancer agents with selective B-RAF V600E /p38α kinase inhibitory activity: Synthesis, in vitro assays and in silico study. |
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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., 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; Pharmaceutical Chemistry Department, Faculty of Pharmacy, Modern University for Technology and Information (MTI), Cairo, 12055, Egypt., Ammar UM; Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, 161 Cathedral Street, Glasgow G4 0NR, Scotland, United Kingdom., 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., Abdel-Maksoud MS; Medicinal & Pharmaceutical Chemistry Department, Pharmaceutical and Drug Industries Research Division, National Research Centre NRC (ID: 60014618)), Dokki, Giza, 12622, Egypt., 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, Mansoura University, Mansoura 35516, Egypt., Haque MM; Department of Pharmacology, College of Medicine, Korea University, Seoul 02841, Republic of Korea., Das T; Biomedical Research Institute, Korea Institute of Science and Technology, Seoul 02792, Republic of Korea., Kim EE; Biomedical Research Institute, Korea Institute of Science and Technology, Seoul 02792, Republic of Korea., Lee JS; Department of Pharmacology, College of Medicine, Korea University, Seoul 02841, 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., 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. Electronic address: hkkim717@jbnu.ac.kr., 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 pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences [Eur J Pharm Sci] 2022 Apr 01; Vol. 171, pp. 106115. Date of Electronic Publication: 2022 Jan 04. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Science B.V Country of Publication: Netherlands NLM ID: 9317982 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1879-0720 (Electronic) Linking ISSN: 09280987 NLM ISO Abbreviation: Eur J Pharm Sci Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Amsterdam : Elsevier Science B.V Original Publication: Amsterdam ; New York : Elsevier, c1993- |
| مواضيع طبية MeSH: | Antineoplastic Agents*/chemistry , Antineoplastic Agents*/pharmacology , Protein Kinase Inhibitors*/chemistry, Animals ; Cell Line, Tumor ; Cell Proliferation ; Dose-Response Relationship, Drug ; Drug Design ; Drug Screening Assays, Antitumor ; Female ; Molecular Structure ; Pyridines/pharmacology ; Structure-Activity Relationship |
| مستخلص: | In the current article, we introduce design of a new series of 4-(imidazol-5-yl)pyridines with improved anticancer activity and selective B-RAF V600E /p38α kinase inhibitory activity. Based on a previous work, a group of structural modifications were applied affording the new potential antiproliferative agents. Towards extensive biological assessment of the target compounds, an in vitro anticancer assay was conducted over NCI 60-cancer cell lines panel representing blood, lung, colon, CNS, skin, ovary, renal, prostate, and breast cancers. Compounds 7c, 7d, 8b, 9b, 9c, 10c, 10d, and 11b exhibited the highest potency among the tested compounds and demonstrated sub-micromolar or one-digit micromolar GI (Copyright © 2022. Published by Elsevier B.V.) |
| فهرسة مساهمة: | Keywords: Anticancer; BRAF(V600E); Cell cycle arrest; Imidazolylpyridine; Molecular modeling; p38α |
| المشرفين على المادة: | 0 (Antineoplastic Agents) 0 (Protein Kinase Inhibitors) 0 (Pyridines) |
| تواريخ الأحداث: | Date Created: 20220107 Date Completed: 20220223 Latest Revision: 20220223 |
| رمز التحديث: | 20240829 |
| DOI: | 10.1016/j.ejps.2022.106115 |
| PMID: | 34995782 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1879-0720 |
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| DOI: | 10.1016/j.ejps.2022.106115 |