ChemRxiv
These are preliminary reports that have not been peer-reviewed. They should not be regarded as conclusive, guide clinical practice/health-related behavior, or be reported in news media as established information. For more information, please see our FAQs.
1/1
2 files

Imide Condensation as a Strategy for the Synthesis of Core Diversified G-Quadruplex Ligands with Anti-Cancer and Anti-Parasitic Activity

preprint
submitted on 09.03.2020, 15:21 and posted on 13.03.2020, 20:16 by 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.

Funding

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.

History

Email Address of Submitting Author

m.c.galan@bristol.ac.uk

Institution

School of Chemistry, University of Bristol

Country

United Kingdom

ORCID For Submitting Author

0000-0001-7307-2871

Declaration of Conflict of Interest

No conflict of interest

Exports

ChemRxiv

Exports