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

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

Volume: 10 Issue: 6

Author(s): Ruben M. Carballo, Leticia G. Leon, Ramiro F. Quijano-Quinones, Gonzalo J. Mena-Rejon, Víctor S. Martin, Jose M. Padron and Juan I. Padron

Affiliation:

Keywords: Antiproliferative activity, aza-cycle, iron catalyst, piperidine, prins cyclization, QSAR.

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 (F05_C-S) of the N-sulfonyl group.

Cite this article as:

Carballo M. Ruben, Leon G. Leticia, Quijano-Quinones F. Ramiro, Mena-Rejon J. Gonzalo, Martin S. Víctor, Padron M. Jose and Padron I. Juan, Antiproliferative Evaluation of N-sulfonyl-2-alkyl-six Membered Azacycles. A QSAR Study, Medicinal Chemistry 2014; 10 (6) . https://dx.doi.org/10.2174/1573406409666131124231552