1338371-93-9Relevant articles and documents
Synthesis and Antileukemic Activity of Novel 4-(3-(Piperidin-4-yl) Propyl)Piperidine Derivatives
Vinaya, Kambappa,Kavitha, Chandagirikoppal V.,Chandrappa, Siddappa,Prasanna, Doddakunche S.,Raghavan, Sathees C.,Rangappa, Kanchugarakoppal S.
experimental part, p. 622 - 630 (2012/04/17)
To explore the anticancer effect associated with the piperidine framework, several (substituted phenyl) {4-[3-(piperidin-4-yl)propyl]piperidin-1-yl} methanone derivatives 3(a-i) were synthesized. Variation in the functional group at N-terminal of the piperidine led to a set of compounds bearing amide moiety. Their chemical structures were confirmed by 1H NMR, IR and mass spectra analysis. Among these, compounds 3a, 3d and 3e were endowed with antiproliferative activity. The most active compound among this series was 3a with nitro and fluoro substitution on the phenyl ring of aryl carboxamide moiety, which inhibited the growth of human leukemia cells (K562 and Reh) at low concentration. Comparison with other derivative (3h) results shown by LDH assay, cell cycle analysis and DNA fragmentation suggested that 3a is more potent to induce apoptosis. Novel (substituted phenyl){4-[3-(piperidin-4-yl)propyl]piperidin-1-yl} methanone derivatives were identified as potent antiproliferative agents. Compound with nitro and fluoro substitution on the phenyl ring of aryl carboxamide moiety was identified as most potent among the series to induce the apoptosis.
