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|Título:||Artemisinin-polypyrrole conjugates: synthesis, DNA binding studies and preliminary antiproliferative evaluation|
|Autor:||La Pensée, Louise|
Chadwick, Amy E.
Araújo, Nuna C.
Cabral, L. I. L.
Cristiano, Maria Lurdes Santos
Wu, Yi Hang
Ward, Stephen A.
Stocks, Paul A.
O'Neill, Paul M.
|Citação:||La Pensée, Louise; Sabbani, Sunil; Sharma, Raman; Bhamra, Inder; Shore, Emma; Chadwick, Amy E.; Berry, Neil G.; Firman, James; Araujo, Nuna C.; Cabral, Lília; Cristiano, Maria L. S.; Bateman, Cerys; Janneh, Omar; Gavrila, Adelina; Wu, Yi Hang; Hussain, Afthab; Ward, Stephen A.; Stocks, Paul A.; Cosstick, Rick; O’Neill, Paul M. Artemisinin-Polypyrrole Conjugates: Synthesis, DNA Binding Studies and Preliminary Antiproliferative Evaluation, ChemMedChem, 8, 5, 709-718, 2013.|
|Resumo:||Artemisinin-based combination therapies (ACTs) are currently the recommended treatment for uncomplicated and severe cases of malaria. Additionally, artemisinins, as well as a number of other sesquiterpene lactones (SLs), are currently in phase I–II clinical trials against breast, colorectal and nonsmall-cell lung cancers. As outlined by the iron-dependent activation hypothesis, the activity of artemisinin (ART) is dependent on the endoperoxide bridge. The peroxide is cleaved by endogenous sources of FeII to generate highly reactive carbon-centred radicals (CCRs), which are believed to react with critical cellular targets. ART demonstrates selectivity towards rapidly proliferating cancer cell lines that possess a high intracellular iron content required to sustain their characteristic high rates of multiplication. Iron activation links this particular potency of ART towards rapidly proliferating cancer cell lines; differentiation between healthy and cancerous cells by variation of iron concentration provides a strategy for selective cytotoxicity by ART and its derivatives. The mechanism by which ART exerts its cytotoxic activity still remains elusive. ART acts by disruption of proliferation,[6, 7] oxidative stress, anti-angiogenesis, NF-kB signalling, apoptosis and interfering with iron uptake and metabolism. ART also induces DNA breakage, and it has been reported that artesunate-mediated DNA damage contributes to its therapeutic efficacy.|
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