Synthesis of New 1,3,5-Triazine-Based 2-Pyrazolines as Potential Anticancer Agents
| Autor: | Rodrigo Abonia, Leydi M. Moreno, Braulio Insuasty, Jairo Quiroga, Jonathan Ramírez-Prada |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2018 |
| Předmět: |
2-pyrazolones
Claisen–Schmidt reaction Hydrazine Pharmaceutical Science Antineoplastic Agents 01 natural sciences Medicinal chemistry Article Analytical Chemistry lcsh:QD241-441 Structure-Activity Relationship 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine 1 3 5-Triazine lcsh:Organic chemistry Cell Line Tumor Drug Discovery cyclocondensation reactions Humans 1 3 5-triazines Physical and Theoretical Chemistry Microwaves microwave irradiation Cell Proliferation Molecular Structure Triazines 010405 organic chemistry Chemistry chalcones Organic Chemistry 0104 chemical sciences Human tumor anticancer activity Chemistry (miscellaneous) 030220 oncology & carcinogenesis Yield (chemistry) Microwave irradiation Pyrazoles Molecular Medicine Amine gas treating Hydrate |
| Zdroj: | Molecules, Vol 23, Iss 8, p 1956 (2018) Molecules Volume 23 Issue 8 Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry |
| ISSN: | 1420-3049 |
| Popis: | A new series of 1,3,5-triazine-containing 2-pyrazoline derivatives (8&ndash 11)a&ndash g was synthesized by cyclocondensation reactions of [(4,6-bis((2-hydroxyethyl)amino)-1,3,5-triazin-2-yl)amine]chalcones 7a&ndash g with hydrazine hydrate and derivatives. Chalcones 7a&ndash g were obtained by Claisen-Schmidt condensation between aromatic aldehydes and triazinic derivative 5, which was synthesized in high yield by a microwave-assisted reaction. Seventeen of the synthesized compounds were selected and tested by the US National Cancer Institute (NCI) for their anticancer activity against 58 different human tumor cell lines. Compounds 7g and 10d,e,g showed important GI50 values ranging from 0.569 to 16.6 µ M and LC50 values ranging from 5.15 to > 100 µ M. |
| Databáze: | OpenAIRE |
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