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

Autor:	Juan Carlos Morales, Gregory Hollingworth, M. Carmen Galan, Michael P. O'Hagan, Pablo Peñalver, Steven T. G. Street
Rok vydání:	2021
Předmět:	chemistry.chemical_compound chemistry Antiparasitic medicine.drug_class Anti parasitic Nucleic acid medicine G-quadruplex Imide Selectivity Antiparasitic agent Combinatorial chemistry DNA
DOI:	10.26434/chemrxiv.11955870
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5ebb1392c744f4c8d2ff1c5f64ca4e38 https://doi.org/10.26434/chemrxiv.11955870 Zobrazit plný text záznamu