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Synthesis of New 1,3,5-Triazine-Based 2-Pyrazolines as Potential Anticancer Agents

A new series of 1,3,5-triazine-containing 2-pyrazoline derivatives (8–11)a–g was synthesized by cyclocondensation reactions of [(4,6-bis((2-hydroxyethyl)amino)-1,3,5-triazin-2-yl)amine]chalcones 7a–g with hydrazine hydrate and derivatives. Chalcones 7a–g were obtained by Claisen-Schmidt condensation...

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Detalles Bibliográficos
Autores principales: Moreno, Leydi M., Quiroga, Jairo, Abonia, Rodrigo, Ramírez-Prada, Jonathan, Insuasty, Braulio
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6222643/
https://www.ncbi.nlm.nih.gov/pubmed/30082588
http://dx.doi.org/10.3390/molecules23081956
Descripción
Sumario:A new series of 1,3,5-triazine-containing 2-pyrazoline derivatives (8–11)a–g was synthesized by cyclocondensation reactions of [(4,6-bis((2-hydroxyethyl)amino)-1,3,5-triazin-2-yl)amine]chalcones 7a–g with hydrazine hydrate and derivatives. Chalcones 7a–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 GI(50) values ranging from 0.569 to 16.6 µM and LC(50) values ranging from 5.15 to >100 µM.