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submitted on 09.03.2020, 15:21 and posted on 13.03.2020, 20:16by Steven T. G. Street, pablo Peñalver, Michael O'Hagan, Gregory J. Hollingworth, Juan Carlos Morales, M. Carmen Galan
A facile imide coupling strategy for the one-step preparation of G‑quadruplex ligands with varied core chemistries is described. The G‑quadruplex stabilization, anticancer and antiparasitic activity of a library of nine compounds was examined, identifying a nanomolar inhibitor of T. brucei with 78‑fold selectivity over MRC5 cells, and strong stabilization of G‑quadruplex nucleic acids.
STGS thanks the EPSRC (EP/G036764/1 and EP/N509619/1) and NSERC, MPO thanks the EPSRC (EP/L015366/1), JCM/PP thank Spanish Ministerio de Ciencia Innovación y Universidades (Grants CTQ2015-64275-P and RTI2018-099036- B-I00) and MCG thanks the European Research Council (ERC-COG: 648239) for funding.