دورية أكاديمية
أعرض في EDS

Design, synthesis and screening of 1, 2, 4-triazinone derivatives as potential antitumor agents with apoptosis inducing activity on MCF-7 breast cancer cell line.

التفاصيل البيبلوغرافية
العنوان: Design, synthesis and screening of 1, 2, 4-triazinone derivatives as potential antitumor agents with apoptosis inducing activity on MCF-7 breast cancer cell line.
المؤلفون: Zaki I; Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Port Said University, Port Said, Egypt., Abdelhameid MK; Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt. Electronic address: mohorganic@hotmail.com., El-Deen IM; Chemistry Department, Faculty of Science, Port Said University, Port Said, Egypt., Abdel Wahab AHA; Cancer Biology Department, National Cancer Institute, Cairo University, Cairo, Egypt., Ashmawy AM; Cancer Biology Department, National Cancer Institute, Cairo University, Cairo, Egypt., Mohamed KO; Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
المصدر: European journal of medicinal chemistry [Eur J Med Chem] 2018 Aug 05; Vol. 156, pp. 563-579. Date of Electronic Publication: 2018 Jul 07.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: Editions Scientifiques Elsevier Country of Publication: France NLM ID: 0420510 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1768-3254 (Electronic) Linking ISSN: 02235234 NLM ISO Abbreviation: Eur J Med Chem Subsets: MEDLINE
أسماء مطبوعة: Publication: Paris : Editions Scientifiques Elsevier
Original Publication: Paris, S.E.C.T. [etc.]
مواضيع طبية MeSH: Drug Design*, Antineoplastic Agents/*chemistry , Antineoplastic Agents/*pharmacology , Apoptosis/*drug effects , Breast Neoplasms/*drug therapy , Triazines/*chemistry , Triazines/*pharmacology, Antineoplastic Agents/chemical synthesis ; Breast Neoplasms/metabolism ; Female ; Humans ; MCF-7 Cells ; Topoisomerase II Inhibitors/chemical synthesis ; Topoisomerase II Inhibitors/chemistry ; Topoisomerase II Inhibitors/pharmacology ; Triazines/chemical synthesis ; Tubulin/metabolism ; Tubulin Modulators/chemical synthesis ; Tubulin Modulators/chemistry ; Tubulin Modulators/pharmacology
مستخلص: Some triazinone derivatives are designed and synthesized as potential antitumor agents. Triazinone derivatives 4c, 5e and 7c show potent anticancer activity over MCF-7 breast cancer cells higher than podophyllotoxin (podo) by approximate 6-fold. DNA flow cytometry analysis for the compounds 3c, 4c, 5e, 6c and 7c show a potent inhibitory activity of cell proliferation and cell cycle arrest at G 2 /M phase. Compounds 4c, 5e and 7c exhibit low to moderate β-tubulin polymerization inhibition percentage. Meanwhile, compound 6c displayed excellent β-tubulin percentage of polymerization inhibition equivalent to that exhibited by podo. In addition, compounds 4c, 5e and 7c show strong topoisomerase (topo) II inhibitory activity in nano-molar concentration, compared to known topo inhibitor as etoposide. Finally, apoptotic inducing activity over MCF-7 of compounds 4c, 5e, 6c and 7c is due to up-regulation of p53, increased Bax/Bcl-2 ratio and caspase3/7 levels 2-fold higher than podo.
(Published by Elsevier Masson SAS.)
المشرفين على المادة: 0 (Antineoplastic Agents)
0 (Topoisomerase II Inhibitors)
0 (Triazines)
0 (Tubulin)
0 (Tubulin Modulators)
تواريخ الأحداث: Date Created: 20180720 Date Completed: 20180904 Latest Revision: 20180904
رمز التحديث: 20231215
DOI: 10.1016/j.ejmech.2018.07.003
PMID: 30025350
قاعدة البيانات: MEDLINE
الوصف
تدمد:1768-3254
DOI:10.1016/j.ejmech.2018.07.003