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Title

Antiproliferative evaluation of N-sulfonyl-2-Alkyl-six membered azacycles. A QSAR study

AuthorsCarballo, Ruben M.; León, Leticia G.; Quijano-Quiñones, Ramiro F.; Mena-Rejón, Gonzalo J.; Martín, Víctor S.; Padrón, José M.; Padrón, Juan I.
KeywordsPiperidine
Iron Catalyst
Prins Cyclization
QSAR
Aza-cycle
Antiproliferative Activity
Issue Date2014
PublisherBentham Science Publishers
CitationMedicinal Chemistry 10(6): 571-579 (2014)
AbstractA 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.
Publisher version (URL)http://dx.doi.org/10.2174/1573406409666131124231552
URIhttp://hdl.handle.net/10261/180313
Identifiersdoi: 10.2174/1573406409666131124231552
issn: 1573-4064
e-issn: 1875-6638
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