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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Authors | Rubén M Carballo, Leticia G León, Ramiro F Quijano-Quiñones, Gonzalo J Mena-Rejón, Víctor S Martín, José M Padrón, Juan I Padrón |
Journal | Medicinal chemistry (Shariqah (United Arab Emirates))
(Med Chem)
Vol. 10
Issue 6
Pg. 571-9
( 2014)
ISSN: 1875-6638 [Electronic] Netherlands |
PMID | 24283219
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Antineoplastic Agents
- Aza Compounds
- Heterocyclic Compounds
- Sulfones
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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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