Synthesis, spectroscopic studies and biological evaluation of acridine derivatives: The role of aggregation on the photodynamic efficiency
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Títol
Synthesis, spectroscopic studies and biological evaluation of acridine derivatives: The role of aggregation on the photodynamic efficiencyAutoria
Data de publicació
2018-03-01Editor
ElsevierISSN
0960-894XCita bibliogràfica
FELIP-LEÓN, Carles, et al. Synthesis, spectroscopic studies and biological evaluation of acridine derivatives: The role of aggregation on the photodynamic efficiency. Bioorganic & medicinal chemistry letters, 2018, vol. 28, no 5, p. 869-874.Tipus de document
info:eu-repo/semantics/articleVersió de l'editorial
https://www.sciencedirect.com/science/article/pii/S0960894X18300866Versió
info:eu-repo/semantics/acceptedVersionParaules clau / Matèries
Resum
Two new photoactive compounds (1 and 2) derived from the 9-amidoacridine chromophore have been synthesized and fully characterized. Their abilities to produce singlet oxygen upon irradiation have been compared. The ... [+]
Two new photoactive compounds (1 and 2) derived from the 9-amidoacridine chromophore have been synthesized and fully characterized. Their abilities to produce singlet oxygen upon irradiation have been compared. The synthesized compounds show very different self-aggregating properties since only 1 present a strong tendency to aggregate in water. Biological assays were conducted with two cell types: hepatoma cells (Hep3B) and human umbilical vein endothelial cells (HUVEC). Photodynamic therapy (PDT) studies carried out with Hep3B cells showed that non-aggregating compound 2 showed photoxicity, ascribed to the production of singlet oxygen, being aggregating compound 1 photochemically inactive. On the other hand suspensions of 1, characterized as nano-sized aggregates, have notable antiproliferative activity towards this cell line in the dark. [-]
Publicat a
Bioorganic & medicinal chemistry letters, 2018, vol. 28, no 5Proyecto de investigación
Ministerio de Economia y Competitividad of Spain: CTQ2015-71004-R; CTQ2012-37735; BES-2013-063296. Universitat Jaume I: P1.1B2015-76Drets d'accés
Copyright © Elsevier B.V.
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info:eu-repo/semantics/openAccess
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info:eu-repo/semantics/openAccess
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