Synthesis, structure, and in vitro anticancer activity of new polycyclic 1,2-diazines
العنوان: | Synthesis, structure, and in vitro anticancer activity of new polycyclic 1,2-diazines |
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المؤلفون: | Vasilichia Bejan, Dorina Mantu, Dan Maftei, Cornelia Ursu, Dorina Iurea |
المصدر: | Medicinal Chemistry Research. 23:2909-2915 |
بيانات النشر: | Springer Science and Business Media LLC, 2013. |
سنة النشر: | 2013 |
مصطلحات موضوعية: | Pyridazine, chemistry.chemical_compound, Chemistry, Stereochemistry, Organic Chemistry, Molecule, General Pharmacology, Toxicology and Pharmaceutics, Phthalazine, Isoindole, Ultrasound irradiation, Benzoquinone, Cycloaddition, In vitro |
الوصف: | The synthesis, structure, and in vitro anticancer activity of a new class of anticancer derivatives with dihydrobenzo[5,6]isoindolo[1,2-a]phthalazine and dihydrobenzo[f]pyridazino[6,1-a]isoindole skeletons are presented. The preparation is straight and efficient, involving two steps only: a N-alkylation of the pyridazine or phthalazine heterocycle, followed by a [3 + 2] dipolar cycloaddition of 1,2-diazinium ylides to the corresponding dipolarophiles. The synthesis was performed under microwave and ultrasound (US) irradiation as well as under conventional thermal heating. The most effective conditions in term of yields and time were found to be US irradiation. The penta- and tetra-cyclic 1,2-diazines were evaluated for their in vitro anticancer activity. The pentacyclic 1,2-diazine derivatives exhibit a significant anticancer activity against Non-Small Cell Lung Cancer NCI-H460, Leukemia MOLT-4, Leukemia CCRF-CEM, and Breast Cancer MCF7. A feasible explanation for anticancer efficiency of the pentacyclic 1,2-diazines have been furnished, being correlated with the mechanisms of action. The synthesis (conventional thermal heating, microwave and ultrasound irradiation), structure, and in vitro anticancer activity of a new class of anticancer molecules with polycyclic 1,2-diazines skeleton is presented. |
تدمد: | 1554-8120 1054-2523 |
URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_________::ed7f3793c3eff00b615008901e797f1a https://doi.org/10.1007/s00044-013-0878-8 |
حقوق: | CLOSED |
رقم الأكسشن: | edsair.doi...........ed7f3793c3eff00b615008901e797f1a |
قاعدة البيانات: | OpenAIRE |
تدمد: | 15548120 10542523 |
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