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Synthesis, characterization, and in vitro SAR evaluation of N,N'-bis(arylmethyl)-C2-alkyl substituted imidazolium salts.


ABSTRACT: A series of C2-alkyl substituted N,N'-bis(arylmethyl)imidazolium salts were synthesized, characterized, and tested for their in vitro anti-cancer activity against multiple non-small cell lung cancer cell lines by our group and the National Cancer Institute's-60 human tumor cell line screen to establish a structure-activity relationship. Compounds are related to previously published N,N'-bis(arylmethyl)imidazolium salts but utilize the historical quinoline motif and anion effects to increase the aqueous solubility. Multiple derivatives displayed high anti-cancer activity with IC50 values in the nanomolar to low micromolar range against a panel of non-small cell lung cancer cell lines. Several of these derivatives have high aqueous solubilities with potent anti-proliferative properties and are ideal candidates for future in vivo xenograft studies and have high potential to progress into clinic use.

SUBMITTER: DeBord MA 

PROVIDER: S-EPMC5204360 | biostudies-literature | 2017 Jan

REPOSITORIES: biostudies-literature

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Synthesis, characterization, and in vitro SAR evaluation of N,N'-bis(arylmethyl)-C<sup>2</sup>-alkyl substituted imidazolium salts.

DeBord Michael A MA   Wagers Patrick O PO   Crabtree Steven R SR   Tessier Claire A CA   Panzner Matthew J MJ   Youngs Wiley J WJ  

Bioorganic & medicinal chemistry letters 20161124 2


A series of C<sup>2</sup>-alkyl substituted N,N'-bis(arylmethyl)imidazolium salts were synthesized, characterized, and tested for their in vitro anti-cancer activity against multiple non-small cell lung cancer cell lines by our group and the National Cancer Institute's-60 human tumor cell line screen to establish a structure-activity relationship. Compounds are related to previously published N,N'-bis(arylmethyl)imidazolium salts but utilize the historical quinoline motif and anion effects to in  ...[more]

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