Abstract
A series of quinazoline-2,4,6-triamine (quinazoline) and 2,6-diaminoquinazolin-4(3H)-one (quinazolinone) derivatives were designed, synthesized and evaluated as cytotoxic agents in three cancer cell lines (HCT-15, SKOV-3, and MDA-MB-231) using conventional MTT assay. Of the tested compounds, only eleven quinazoline derivatives showed activity against all the tested cell lines, at 24 h of exposure. Among them, the compounds 3e and 3f exhibited the highest cytotoxic activity, with the most important IC50 values ranging from 4.5 to 15.5 μM. They were more active than the reference drugs (Gefitinib, PD153035) which showed IC50 values ranging between 19.4 and 48.8 μM. These compounds open new possibilities for preparing novel analogous of quinazoline as antitumor agents.
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Acknowledgements
This study was sponsored by grants from UNAM-DGAPA-PAPIIT IN218117 and CONACYT-CB220664. We are grateful to Rosa Isela del Villar, Nayeli López and Marisela Gutiérrez from Facultad de Química, USAI, UNAM for the determination of IR and NMR spectra. Also, we thank to Geiser Cuéllar-Rivera, from Department of Chemistry of the CINVESTAV, for the analytical support in the mass spectrometry; Adriana-Guadalupe Pérez-Ruiz for assisting with the counseling of biological tests; Abimael Mondragón-Peralta for assisting with the biological evaluation; José Fausto Rivero-Cruz for his technical assistance.
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Matus-Meza, A.S., Velasco-Velázquez, M.A. & Hernández-Luis, F. Design, synthesis and cytotoxic evaluation of quinazoline-2,4,6-triamine and 2,6-diaminoquinazolin-4(3H)-one derivatives. Med Chem Res 27, 1748–1756 (2018). https://doi.org/10.1007/s00044-018-2188-7
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DOI: https://doi.org/10.1007/s00044-018-2188-7