%0 Journal Article
%A Lorente-Macías, Álvaro
%A Iañez, Inmaculada
%A Jiménez-López, M Carmen
%A Benítez-Quesada, Manuel
%A Torres-Rusillo, Sara
%A Díaz-Mochón, Juan J
%A Molina, Ignacio J
%A Pineda de Las Infantas, María J
%T Synthesis and screening of 6-alkoxy purine analogs as cell type-selective apoptotic inducers in Jurkat cells.
%D 2021
%U https://hdl.handle.net/10668/27669
%X 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-9H-purine (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.
%K anticancer drugs
%K apoptosis
%K leukemia
%K phenotypic screening
%K purine analogs
%~