دورية أكاديمية
Design and synthesis of novel quinazoline nitrogen mustard derivatives as potential therapeutic agents for cancer.
| العنوان: | Design and synthesis of novel quinazoline nitrogen mustard derivatives as potential therapeutic agents for cancer. |
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| المؤلفون: | Li S; Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China., Wang X, He Y, Zhao M, Chen Y, Xu J, Feng M, Chang J, Ning H, Qi C |
| المصدر: | European journal of medicinal chemistry [Eur J Med Chem] 2013 Sep; Vol. 67, pp. 293-301. Date of Electronic Publication: 2013 Jul 04. |
| نوع المنشور: | Journal Article; Research Support, Non-U.S. Gov't |
| 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/*chemical synthesis , Antineoplastic Agents/*pharmacology , Mechlorethamine/*pharmacology , Quinazolines/*pharmacology, Antineoplastic Agents/chemistry ; Apoptosis/drug effects ; Cell Cycle/drug effects ; Cell Line ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Hep G2 Cells ; Humans ; MCF-7 Cells ; Mechlorethamine/chemical synthesis ; Mechlorethamine/chemistry ; Molecular Structure ; Quinazolines/chemical synthesis ; Quinazolines/chemistry ; Structure-Activity Relationship |
| مستخلص: | Thirteen novel quinazoline nitrogen mustard derivatives were designed, synthesized and evaluated for their anticancer activities in vitro and in vivo. Cytotoxicity assays were carried out in five cancer cell lines (HepG2, SH-SY5Y, DU145, MCF-7 and A549) and one normal human cell line (GES-1), in which compound 22b showed very low IC50 to HepG2 (the IC50 value is 3.06 μM), which was lower than Sorafenib. Compound 22b could inhibit cell cycle at S and G2/M phase and induce cell apoptosis. In the HepG2 xenograft model, 22b exhibited significant cancer growth inhibition with low host toxicity in vivo. (Copyright © 2013 Elsevier Masson SAS. All rights reserved.) |
| فهرسة مساهمة: | Keywords: (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide; 4-dimethylaminopyridine; A549; Anticancer; Apoptosis; Cell cycle; DMAP; DU145; FBS; HCC; HepG2; MCF-7; MTT; Nitrogen mustard; PBS; PI; Quinazoline; RNase A; SH-SY5Y; Xenograft model; fetal bovine serum; hepatic carcinoma; human alveolar adenocarcinoma cell line; human breast cancer cell line; human liver carcinoma cell line; human neuroblastoma cell line; human prostate cancer cell lines; phosphate buffer solution; propidium iodide; ribonuclease A |
| المشرفين على المادة: | 0 (Antineoplastic Agents) 0 (Quinazolines) 50D9XSG0VR (Mechlorethamine) |
| تواريخ الأحداث: | Date Created: 20130723 Date Completed: 20140404 Latest Revision: 20151119 |
| رمز التحديث: | 20240628 |
| DOI: | 10.1016/j.ejmech.2013.06.055 |
| PMID: | 23871909 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1768-3254 |
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| DOI: | 10.1016/j.ejmech.2013.06.055 |