دورية أكاديمية
Development of chromone-thiazolidine-2,4-dione Knoevenagel conjugates as apoptosis inducing agents.
| العنوان: | Development of chromone-thiazolidine-2,4-dione Knoevenagel conjugates as apoptosis inducing agents. |
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| المؤلفون: | Galla MS; Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India., Kale NB; Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India., Sharma A; Department of Biological Sciences, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India., Hajare A; Department of Biological Sciences, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India., Godugu C; Department of Biological Sciences, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India., Shankaraiah N; Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India. Electronic address: shankar@niperhyd.ac.in. |
| المصدر: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2024 Sep 01; Vol. 109, pp. 129853. Date of Electronic Publication: 2024 Jun 21. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Oxford : Elsevier Science Ltd Original Publication: Oxford ; New York : Pergamon Press, c1991- |
| مواضيع طبية MeSH: | Apoptosis*/drug effects , Chromones*/pharmacology , Chromones*/chemistry , Chromones*/chemical synthesis , Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/chemistry , Antineoplastic Agents*/chemical synthesis , Thiazolidinediones*/pharmacology , Thiazolidinediones*/chemistry , Thiazolidinediones*/chemical synthesis , Cell Proliferation*/drug effects , Drug Screening Assays, Antitumor*, Humans ; Structure-Activity Relationship ; Molecular Structure ; Dose-Response Relationship, Drug ; Molecular Docking Simulation ; HEK293 Cells ; Proto-Oncogene Proteins c-bcl-2/metabolism ; Cell Line, Tumor |
| مستخلص: | Overexpression of Bcl-2 protein is a predominant hallmark of disturbed apoptotic pathway in most of the cancers. Herein, chromone-linked thiazolidinediones were designed and synthesized to target Bcl-2 for regulating anti-apoptotic proteins. The study on in vitro cancer cell lines revealed the presence of compounds 8a, 8k, 8l, and 8n, which were found to have good to moderate anti-proliferative activity (with an 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 Ltd. All rights reserved.) |
| فهرسة مساهمة: | Keywords: Anticancer; Apoptosis; Bcl-2; Chromone; Knoevenagel condensation; Thiazolidinedione |
| المشرفين على المادة: | 0 (Chromones) 0 (Antineoplastic Agents) 0 (Thiazolidinediones) 0 (thiazolidine-2,4-dione) 0 (Proto-Oncogene Proteins c-bcl-2) |
| تواريخ الأحداث: | Date Created: 20240623 Date Completed: 20240630 Latest Revision: 20240711 |
| رمز التحديث: | 20240712 |
| DOI: | 10.1016/j.bmcl.2024.129853 |
| PMID: | 38909705 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1464-3405 |
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| DOI: | 10.1016/j.bmcl.2024.129853 |