RT Journal Article
T1 Synthesis and screening of 6-alkoxy purine analogs as cell type-selective apoptotic inducers in Jurkat cells.
A1 Lorente-Macías, Álvaro
A1 Iañez, Inmaculada
A1 Jiménez-López, M Carmen
A1 Benítez-Quesada, Manuel
A1 Torres-Rusillo, Sara
A1 Díaz-Mochón, Juan J
A1 Molina, Ignacio J
A1 Pineda de Las Infantas, María J
K1 anticancer drugs
K1 apoptosis
K1 leukemia
K1 phenotypic screening
K1 purine analogs
AB 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.
YR 2021
FD 2021-06-15
LK https://hdl.handle.net/10668/27669
UL https://hdl.handle.net/10668/27669
LA en
DS RISalud
RD Apr 14, 2025