Synthesis, structure, and in vitro anticancer activity of new polycyclic 1,2-diazines

التفاصيل البيبلوغرافية
العنوان: Synthesis, structure, and in vitro anticancer activity of new polycyclic 1,2-diazines
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