دورية أكاديمية
Discovery of novel benzimidazole derivatives as potent HDACs inhibitors against leukemia with (Thio)Hydantoin as zinc-binding moiety: Design, synthesis, enzyme inhibition, and cellular mechanistic study.
| العنوان: | Discovery of novel benzimidazole derivatives as potent HDACs inhibitors against leukemia with (Thio)Hydantoin as zinc-binding moiety: Design, synthesis, enzyme inhibition, and cellular mechanistic study. |
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| المؤلفون: | Abdulwahab HG; Department of Pharmaceutical Medicinal Chemistry and Drug Design, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt. Electronic address: hanangaber@azhar.edu.eg., Mansour RE; Department of Pharmaceutical Medicinal Chemistry and Drug Design, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt., Farghaly TA; Department of Chemistry, Faculty of Applied Science, Umm Al-Qura University, Makkah, Saudi Arabia. Electronic address: tamohamed@uqu.edu.sa., El-Sehrawi HM; Department of Pharmaceutical Medicinal Chemistry and Drug Design, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt. |
| المصدر: | Bioorganic chemistry [Bioorg Chem] 2024 May; Vol. 146, pp. 107284. Date of Electronic Publication: 2024 Mar 13. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Country of Publication: United States NLM ID: 1303703 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1090-2120 (Electronic) Linking ISSN: 00452068 NLM ISO Abbreviation: Bioorg Chem Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Amsterdam : Elsevier Original Publication: New York, London, Academic Press. |
| مواضيع طبية MeSH: | Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/chemistry , Hydantoins*/pharmacology , Leukemia*/drug therapy, Humans ; Cell Line, Tumor ; Cell Proliferation ; Histone Deacetylase Inhibitors/pharmacology ; Histone Deacetylase Inhibitors/chemistry ; Histone Deacetylases/metabolism ; Histones/metabolism ; Molecular Docking Simulation ; Structure-Activity Relationship ; Zinc/metabolism ; Benzimidazoles/chemistry ; Benzimidazoles/pharmacology |
| مستخلص: | Based on the well-established pharmacophoric features required for histone deacetylase (HDAC) inhibition, a novel series of easy-to-synthesize benzimidazole-linked (thio)hydantoin derivatives was designed and synthesized as HDAC6 inhibitors. All target compounds potently inhibited HDAC6 at nanomolar levels with compounds 2c, 2d, 4b and 4c (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 © 2024 Elsevier Inc. All rights reserved.) |
| فهرسة مساهمة: | Keywords: (Thio)hydantoin; Benzimidazole; Cytotoxicity; HDAC6 inhibitor; Leukemia |
| المشرفين على المادة: | 0 (Antineoplastic Agents) 0 (Histone Deacetylase Inhibitors) EC 3.5.1.98 (Histone Deacetylases) 0 (Histones) 0 (Hydantoins) J41CSQ7QDS (Zinc) 0 (Benzimidazoles) |
| تواريخ الأحداث: | Date Created: 20240317 Date Completed: 20240415 Latest Revision: 20240503 |
| رمز التحديث: | 20240503 |
| DOI: | 10.1016/j.bioorg.2024.107284 |
| PMID: | 38493640 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1090-2120 |
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| DOI: | 10.1016/j.bioorg.2024.107284 |