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Updated: May 5, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Antiproliferative evaluation of N-sulfonyl-2-alkyl-six membered azacycles. A QSAR study
Rubén M Carballo, Leticia G León, Ramiro F Quijano-Quiñones
1Instituto de Productos Naturales y Agrobiologia, CSIC, C/Astrofisico Francisco Sanchez 3, 38206 La Laguna, Spain. jipadron@ipna.csic.es.
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.
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