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Design, Synthesis and In Vitro Activity of Anticancer Styrylquinolines. The p53 Independent Mechanism of Action.

التفاصيل البيبلوغرافية
العنوان: Design, Synthesis and In Vitro Activity of Anticancer Styrylquinolines. The p53 Independent Mechanism of Action.
المؤلفون: Anna Mrozek-Wilczkiewicz, Ewelina Spaczynska, Katarzyna Malarz, Wioleta Cieslik, Marzena Rams-Baron, Vladimír Kryštof, Robert Musiol
المصدر: PLoS ONE, Vol 10, Iss 11, p e0142678 (2015)
بيانات النشر: Public Library of Science (PLoS), 2015.
سنة النشر: 2015
المجموعة: LCC:Medicine
LCC:Science
مصطلحات موضوعية: Medicine, Science
الوصف: A group of styrylquinolines were synthesized and tested for their anti-proliferative activity. Anti-proliferative activity was evaluated against the human colon carcinoma cell lines that had a normal expression of the p53 protein (HCT116 p53+/+) and mutants with a disabled TP53 gene (HCT116 p53-/-) and against the GM 07492 normal human fibroblast cell line. A SAR study revealed the importance of Cl and OH as substituents in the styryl moiety. Several of the compounds that were tested were found to have a marked anti-proliferative activity that was similar to or better than doxorubicin and were more active against the p53 null than the wild type cells. The cellular localization tests and caspase activity assays suggest a mechanism of action through the mitochondrial pathway of apoptosis in a p53-independent manner. The activity of the styrylquinoline compounds may be associated with their DNA intercalating ability.
نوع الوثيقة: article
وصف الملف: electronic resource
اللغة: English
تدمد: 1932-6203
Relation: http://europepmc.org/articles/PMC4657899?pdf=render; https://doaj.org/toc/1932-6203
DOI: 10.1371/journal.pone.0142678
URL الوصول: https://doaj.org/article/8a682671dd024e808d5363235890eadc
رقم الأكسشن: edsdoj.8a682671dd024e808d5363235890eadc
قاعدة البيانات: Directory of Open Access Journals
الوصف
تدمد:19326203
DOI:10.1371/journal.pone.0142678