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

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.
AuthorsRubén M Carballo, Leticia G León, Ramiro F Quijano-Quiñones, Gonzalo J Mena-Rejón, Víctor S Martín, José M Padrón, Juan I Padrón
JournalMedicinal chemistry (Shariqah (United Arab Emirates)) (Med Chem) Vol. 10 Issue 6 Pg. 571-9 ( 2014) ISSN: 1875-6638 [Electronic] Netherlands
PMID24283219 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antineoplastic Agents
  • Aza Compounds
  • Heterocyclic Compounds
  • Sulfones
Topics
  • Antineoplastic Agents (chemistry, pharmacology)
  • Aza Compounds (chemistry, pharmacology)
  • Cell Line, Tumor
  • Cell Proliferation (drug effects)
  • Heterocyclic Compounds (chemistry, pharmacology)
  • Humans
  • Quantitative Structure-Activity Relationship
  • Sulfones (chemistry, pharmacology)

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