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Synthesis of novel naphthoquinone-spermidine conjugates and their effects on DNA-topoisomerases I and II-alpha

التفاصيل البيبلوغرافية
العنوان: Synthesis of novel naphthoquinone-spermidine conjugates and their effects on DNA-topoisomerases I and II-alpha
المؤلفون: Cunha Andréa S., Lima Edson L. S., Pinto Angelo C., Esteves-Souza Andressa, Echevarria Aurea, Camara Celso A., Vargas Maria D., Torres José C.
المصدر: Journal of the Brazilian Chemical Society, Vol 17, Iss 3, Pp 439-442 (2006)
بيانات النشر: Sociedade Brasileira de Química, 2006.
سنة النشر: 2006
المجموعة: LCC:Chemistry
مصطلحات موضوعية: spermidine, lapachol, lawsone, nor-lapachol, DNA-topoisomerase II-alpha, Chemistry, QD1-999
الوصف: Novel derivatives of lapachol 2, nor-lapachol 3 and lawsone 4 have been synthesized by nucleophilic displacement of the methoxynaphthoquinones 2a, 3a and 4a with the polyamine (PA) N¹-Boc-N5-Bn-spermidine 1a. The respective products 2b-4b were obtained in good yields and characterized by spectroscopic and analytical methods. The inhibitory action of these naphthoquinone-PA conjugates on DNA-topoisomerases (topo) I and II-alpha was evaluated by relaxation assay of supercoiled DNA plasmid. All compounds (1a 2b, 3b and 4b) presented significant inhibition of topo II-alpha catalytic activity at the 2 µM dose. Considering that only PA 1a did not inhibit the enzyme catalytic activity at the 0.2 µM dose, the appended naphthoquinone moiety acts as a "value added" fragment. Compounds 1a 2b, 3b and 4b did not inhibit the enzyme DNA-topo I at the 200 µM dose.
نوع الوثيقة: article
وصف الملف: electronic resource
اللغة: English
تدمد: 0103-5053
1678-4790
Relation: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532006000300002; https://doaj.org/toc/0103-5053; https://doaj.org/toc/1678-4790
URL الوصول: https://doaj.org/article/3e6f057ec65b48aba49f68ea8a9d7508
رقم الأكسشن: edsdoj.3e6f057ec65b48aba49f68ea8a9d7508
قاعدة البيانات: Directory of Open Access Journals
الوصف
تدمد:01035053
16784790