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Título: | Antiproliferative evaluation of N-sulfonyl-2-Alkyl-six membered azacycles. A QSAR study |
Autor: | Carballo, Rubén M.; León, Leticia G.; Quijano-Quiñones, Ramiro F.; Mena-Rejón, Gonzalo J.; Martín, Víctor S. CSIC ORCID; Padrón, José M.; Padrón, Juan I. CSIC ORCID | Palabras clave: | Piperidine Iron Catalyst Prins Cyclization QSAR Aza-cycle Antiproliferative activity |
Fecha de publicación: | 2014 | Editor: | Bentham Science Publishers | Citación: | Medicinal Chemistry 10(6): 571-579 (2014) | Resumen: | A series of functionalized N-sulfonyl-piperidines and N-sulfonyl-tetrahydropyridines were evaluated for their antiproliferative activity against the representative panel of human solid tumor cells A2780 (ovarian), SW1573 (non-small cell lung) and WiDr (colon). The SAR study showed for WiDr cells a correlation between the biological activity and the length of the N-sulfonyl group, the nature of the substituents and the type of alkyl side chain. Further QSAR studies indicate that the size and nature of the N-sulfonyl group, the atomic polarizability (MP) and the partition coefficient are the most important descriptors for the activity. The major contribution is the size (F05C-S) of the N-sulfonyl group. | Versión del editor: | http://dx.doi.org/10.2174/1573406409666131124231552 | URI: | http://hdl.handle.net/10261/180313 | DOI: | 10.2174/1573406409666131124231552 | Identificadores: | doi: 10.2174/1573406409666131124231552 issn: 1573-4064 e-issn: 1875-6638 |
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