Synthesis and screening of 6‐alkoxy purine analogs as cell type‐selective apoptotic inducers in Jurkat cells
Metadatos
Mostrar el registro completo del ítemAutor
Lorente Macías, Álvaro; Iáñez García, Inmaculada; Jiménez López, M. Carmen; Benítez Quesada, Manuel; Torres Rusillo, Sara; Díaz Mochón, Juan José; Molina Pineda Infantas, Ignacio Jesús; Pineda De Las Infant Y Villatoro, María JoséEditorial
Wiley-VCH Verlag GmbH
Materia
Anticancer drugs Apoptosis Leukemia Phenotypic screening Purine analogs
Fecha
2021-06-15Referencia bibliográfica
Á. Lorente‐Macías... [et al.]. Synthesis and screening of 6‐alkoxy purine analogs as cell type‐selective apoptotic inducers in Jurkat cells. Arch. Pharm. 2021, e2100095. [https://doi.org/10.1002/ardp.202100095]
Patrocinador
Instituto de Salud Carlos III Spanish Government European Commission RTC-2017-6620; Ministerio de Educacion, Cultura y Deporte FPU 14/00818Resumen
Purines are ubiquitous structures in cell biology involved in a multitude of cellular
processes, because of which substituted purines and analogs are considered
excellent scaffolds in drug design. In this study, we explored the key structural
features of a purine‐based proapoptotic hit, 8‐tert‐butyl‐9‐phenyl‐6‐benzyloxy‐9Hpurine
(1), by setting up a library of 6‐alkoxy purines with the aim of elucidating the
structural requirements that govern its biological activity and to study the cell
selectivity of this chemotype. This was done by a phenotypic screening approach
based on cell cycle analysis of a panel of six human cancer cell lines, including T cell
leukemia Jurkat cells. From this study, two derivatives (12 and 13) were identified
as Jurkat‐selective proapoptotic compounds, displaying superior potency and cell
selectivity than hit 1.