Structure-activity relationship studies on divalent naphthalene diimide G quadruplex ligands with anticancer and antiparasitic activity

Manuel Pérez-Soto,Pablo Peñalver,Steven T G Street, Dora Weenink,Michael P O'Hagan,Javier Ramos-Soriano, Y Jennifer Jiang,Gregory J Hollingworth,M Carmen Galan,Juan C Morales

Bioorganic & Medicinal Chemistry（2022）

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摘要

•Synthesis of new G-quadruplex ligands based on naphthalene diimide (NDI).•Structure activity relationships keeping NDI and modifying spacer and cationic groups.•Testing the in vitro anticancer and antiparasitic activity.•N-methylpiperazine NDIs with flexible linkers were the best G4 ligands.•Found a dimorpholine NDI as the best candidate against T.brucei.

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关键词

G-quadruplex,Ligand,Naphthalene diimide,Antiproliferative,Antiparasitic

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