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Medicinal Chemistry
ISSN (Print): 1573-4064
ISSN (Online): 1875-6638
Epub Full Text Article
DOI: 10.2174/1573406409666131124231552      Price:  $95









Antiproliferative Evaluation of N-sulfonyl-2-alkyl-six Membered Azacycles. A QSAR Study

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Author(s): Rubén M. Carballo, Leticia G. León, Ramiro F. Quijano-Quiñones, Gonzalo J. Mena-Rejón, Víctor S. Martín, José M. Padrón and Juan I. Padrón
Abstract:
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
Keywords:
Antiproliferative Activity, aza-cycle, Iron Catalyst, Piperidine, Prins cyclization, QSAR
Affiliation:
Instituto de Productos Naturales y Agrobiología, CSIC C/Astrofísico Francisco Sánchez 338206 La Laguna, Spain