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http://hdl.handle.net/1843/76405| Type: | Artigo de Periódico |
| Title: | Highly functionalized piperidines: free radical scavenging, anticancer activity, dna interaction and correlation with biological activity |
| Authors: | Suvankar Das Isis Martins Figueiredo Edeildo Ferreira da Silva-Júnior Thiago Mendonça de Aquino João Xavier de Araújo-Júnior Goutam Brahmachari Luzia Valentina Modolo Cristiane Jovelina da Silva Marina de Magalhães Silva Maria Dayanne de Araújo Dantas Ângelo de Fátima Ana Lucia Tasca Gois Ruiz Cleiton Moreira da Silva João Ernesto de Carvalho Josué Carinhanha Caldas Santos |
| Abstract: | Twenty-five piperidines were studied as potential radical scavengers and antitumor agents. Quantitative interaction of compounds with ctDNA using spectroscopic techniques was also evaluated. Our results demonstrate that the evaluated piperidines possesses different abilities to scavenge the radical 2,2-diphenyl-1-picrylhydrazyl (DPPH) and the anion radical superoxide (radical dotO2−). The piperidine 19 was the most potent radical DPPH scavenger, while the most effective to radical dotO2− scavenger was piperidine 10. In general, U251, MCF7, NCI/ADR-RES, NCI-H460 and HT29 cells were least sensitive to the tested compounds and all compounds were considerably more toxic to the studied cancer cell lines than to the normal cell line HaCaT. The binding mode of the compounds and ctDNA was preferably via intercalation. In addition, these results were confirmed based on theoretical studies. Finally, a linear and exponential correlation between interaction constant (Kb) and GI50 for several human cancer cell was observed. |
| Subject: | Agentes antineoplásicos DNA Reações de radicais livres Compostos heterocíclicos |
| language: | eng |
| metadata.dc.publisher.country: | Brasil |
| Publisher: | Universidade Federal de Minas Gerais |
| Publisher Initials: | UFMG |
| metadata.dc.publisher.department: | ICB - DEPARTAMENTO DE BOTÂNICA ICX - DEPARTAMENTO DE QUÍMICA |
| Rights: | Acesso Aberto |
| metadata.dc.identifier.doi: | https://doi.org/10.1016/j.jare.2017.10.010 |
| URI: | http://hdl.handle.net/1843/76405 |
| Issue Date: | 2018 |
| metadata.dc.url.externa: | https://www.sciencedirect.com/science/article/pii/S2090123217301145 |
| metadata.dc.relation.ispartof: | Journal of Advanced Research |
| Appears in Collections: | Artigo de Periódico |
Files in This Item:
| File | Description | Size | Format | |
|---|---|---|---|---|
| Highly functionalized piperidines Free radical scavenging, anticancer.pdf | 1.12 MB | Adobe PDF | View/Open |
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