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Synthesis, characterization, in vitro SAR study, and preliminary in vivo toxicity evaluation of naphthylmethyl substituted bis-imidazolium salts.

Authors:
Marie R Southerland Michael A DeBord Nicholas A Johnson Steven R Crabtree Nicolas E Alexander Michael L Stromyer Patrick O Wagers Matthew J Panzner Chrys Wesdemiotis Leah P Shriver Claire A Tessier Wiley J Youngs

Bioorg Med Chem 2021 Jan 28;30:115893. Epub 2020 Nov 28.

Department of Chemistry, The University of Akron, Akron, OH 44325-3601, USA. Electronic address:

A series of novel bis-imidazolium salts was synthesized, characterized, and evaluated in vitro against a panel of non-small cell lung cancer (NSCLC) cells. Two imidazolium cores were connected with alkyl chains of varying lengths to develop a structure activity relationship (SAR). Increasing the length of the connecting alkyl chain was shown to correlate to an increase in the anti-proliferative activity. The National Cancer Institute's NCI-60 human tumor cell line screen confirmed this trend. The compound containing a decyl linker chain, 10, was chosen for further in vivo toxicity studies with C578BL/6 mice. The compound was well tolerated by the mice and all of the animals survived and gained weight over the course of the study.

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Source
http://dx.doi.org/10.1016/j.bmc.2020.115893DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7903221PMC
January 2021

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