دورية أكاديمية
Novel 2-[thio]acetamide linked quinazoline/1,2,4-triazole/chalcone hybrids: Design, synthesis, and anticancer activity as EGFR inhibitors and apoptotic inducers.
العنوان: | Novel 2-[thio]acetamide linked quinazoline/1,2,4-triazole/chalcone hybrids: Design, synthesis, and anticancer activity as EGFR inhibitors and apoptotic inducers. |
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المؤلفون: | Abdelkhalek AS; Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt., Kothayer H; Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt., Soltan MK; Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt.; Pharmacy Program, Oman College of Health Sciences, Muscat, Sultanate of Oman., Ibrahim SM; Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt., Elbaramawi SS; Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt. |
المصدر: | Archiv der Pharmazie [Arch Pharm (Weinheim)] 2024 Jul; Vol. 357 (7), pp. e2300627. Date of Electronic Publication: 2024 Apr 09. |
نوع المنشور: | Journal Article |
اللغة: | English |
بيانات الدورية: | Publisher: Wiley-VCH Verlag GmbH & Co. KGaA Country of Publication: Germany NLM ID: 0330167 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1521-4184 (Electronic) Linking ISSN: 03656233 NLM ISO Abbreviation: Arch Pharm (Weinheim) Subsets: MEDLINE |
أسماء مطبوعة: | Publication: <2005->: Weinheim Germany : Wiley-VCH Verlag GmbH & Co. KGaA Original Publication: Weinheim, Verlag Chemie GmbH. |
مواضيع طبية MeSH: | ErbB Receptors*/antagonists & inhibitors , ErbB Receptors*/metabolism , Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/chemical synthesis , Antineoplastic Agents*/chemistry , Apoptosis*/drug effects , Quinazolines*/pharmacology , Quinazolines*/chemistry , Quinazolines*/chemical synthesis , Drug Design* , Cell Proliferation*/drug effects , Triazoles*/pharmacology , Triazoles*/chemistry , Triazoles*/chemical synthesis , Drug Screening Assays, Antitumor* , Molecular Docking Simulation* , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/chemical synthesis , Protein Kinase Inhibitors*/chemistry, Humans ; Structure-Activity Relationship ; Cell Line, Tumor ; Molecular Structure ; Dose-Response Relationship, Drug ; Chalcones/pharmacology ; Chalcones/chemical synthesis ; Chalcones/chemistry ; HCT116 Cells ; Acetamides/pharmacology ; Acetamides/chemistry ; Acetamides/chemical synthesis ; MCF-7 Cells ; Chalcone/pharmacology ; Chalcone/chemistry ; Chalcone/chemical synthesis |
مستخلص: | Novel triazoloquinazolines carrying the 2-[thio]acetamide entity (4 and 5a-d) and triazoloquinazoline/chalcone hybrids incorporating the 2-[thio]acetamide linker (8a-b and 9a-f) were developed as anticancer candidates. NCI screening of the synthesized compounds at 10 μM concentration displayed growth inhibition not only up to 99.74% as observed for 9a but also a lethal effect could be achieved as stated for compounds 9c (RPMI-8226 and HCT-116) and 8b, 9a, and 9e on the HCT-116 cell line. The antiproliferative activity was determined for the chalcone series on three cell lines: RPMI-8226, HCT-116, and MCF-7. Compounds 8b, 9a, 9b, and 9f were the most active ones. To understand the mechanistic study, the inhibitory effect on the epidermal growth factor receptor (EGFR) kinase was evaluated. The results stated that the activity of compound 8b (IC (© 2024 Deutsche Pharmazeutische Gesellschaft.) |
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فهرسة مساهمة: | Keywords: EGFR inhibitors; apoptotic inducers; chalcone; dual activity; triazoloquinazoline hybrids |
المشرفين على المادة: | EC 2.7.10.1 (ErbB Receptors) 0 (Antineoplastic Agents) 0 (Quinazolines) EC 2.7.10.1 (EGFR protein, human) 0 (Triazoles) 0 (Protein Kinase Inhibitors) 0 (Chalcones) 288-88-0 (1,2,4-triazole) 0 (Acetamides) 5S5A2Q39HX (Chalcone) |
تواريخ الأحداث: | Date Created: 20240409 Date Completed: 20240703 Latest Revision: 20240709 |
رمز التحديث: | 20240709 |
DOI: | 10.1002/ardp.202300627 |
PMID: | 38593298 |
قاعدة البيانات: | MEDLINE |
تدمد: | 1521-4184 |
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DOI: | 10.1002/ardp.202300627 |