دورية أكاديمية
Design, synthesis and molecular modeling study of certain 4-Methylbenzenesulfonamides with CDK2 inhibitory activity as anticancer and radio-sensitizing agents.
| العنوان: | Design, synthesis and molecular modeling study of certain 4-Methylbenzenesulfonamides with CDK2 inhibitory activity as anticancer and radio-sensitizing agents. |
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| المؤلفون: | Ghorab MM; Department of Drug Radiation Research, National Centre for Radiation Research and Technology (NCRRT), Egyptian Atomic Energy Authority (EAEA), PO box 29, Nasr City, Cairo, Egypt. Electronic address: mmsghorab@yahoo.com., Ragab FA; Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmacy, Cairo University, Cairo, Egypt., Heiba HI; Department of Drug Radiation Research, National Centre for Radiation Research and Technology (NCRRT), Egyptian Atomic Energy Authority (EAEA), PO box 29, Nasr City, Cairo, Egypt., Elsayed MSA; Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and the Purdue Center for Cancer Research, Purdue University, West Lafayette, IN 47907, United States., Ghorab WM; Department of Drug Radiation Research, National Centre for Radiation Research and Technology (NCRRT), Egyptian Atomic Energy Authority (EAEA), PO box 29, Nasr City, Cairo, Egypt. |
| المصدر: | Bioorganic chemistry [Bioorg Chem] 2018 Oct; Vol. 80, pp. 276-287. Date of Electronic Publication: 2018 Jun 05. |
| 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: | Drug Design*, Antineoplastic Agents/*chemical synthesis , Cyclin-Dependent Kinase 2/*metabolism , Protein Kinase Inhibitors/*chemical synthesis , Sulfonamides/*chemistry , Toluene/*analogs & derivatives, Antineoplastic Agents/metabolism ; Antineoplastic Agents/pharmacology ; Binding Sites ; Catalytic Domain ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Cyclin-Dependent Kinase 2/antagonists & inhibitors ; Drug Screening Assays, Antitumor ; Gamma Rays ; Humans ; Molecular Docking Simulation ; Protein Kinase Inhibitors/metabolism ; Protein Kinase Inhibitors/pharmacology ; Structure-Activity Relationship ; Sulfonamides/metabolism ; Sulfonamides/pharmacology ; Toluene/chemistry ; Toluene/metabolism ; Toluene/pharmacology |
| مستخلص: | Two series of 2-aminopyridine derivatives 6-17 and tyrphostin AG17 analogs 18-22 bearing 4-methylbenzenesulfonamide moiety were designed and synthesized as anticancer compounds. The synthesized compounds were biologically evaluated for their cytotoxic activity against human breast cancer cell line MCF-7. From 2-aminopyridine and tyrphostin AG17 series, compounds 14, 16 and 20 showed the best activities with IC (Copyright © 2018 Elsevier Inc. All rights reserved.) |
| فهرسة مساهمة: | Keywords: 2-Aminopyridine; 4-methylbenzenesulfonamide; CDK2; Cytotoxic; Tyrphostin AG17 analogs; γ-radiation |
| المشرفين على المادة: | 0 (Antineoplastic Agents) 0 (Protein Kinase Inhibitors) 0 (Sulfonamides) 3FPU23BG52 (Toluene) EC 2.7.11.22 (CDK2 protein, human) EC 2.7.11.22 (Cyclin-Dependent Kinase 2) I8266RI90M (4-toluenesulfonamide) |
| تواريخ الأحداث: | Date Created: 20180704 Date Completed: 20190422 Latest Revision: 20190422 |
| رمز التحديث: | 20240628 |
| DOI: | 10.1016/j.bioorg.2018.06.010 |
| PMID: | 29966874 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1090-2120 |
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| DOI: | 10.1016/j.bioorg.2018.06.010 |