2‐Ethenyl Imidazolium Salts: Synthesis, Characterization, and Evaluation as Potential Chemotherapeutics

Author:

Hobbs Mahala S.1,Chen Wei‐Yuan1,Youngs Wiley J.1,Ziegler Christopher J.1ORCID

Affiliation:

1. Department of Chemistry, University of Akron Akron, OH 44321 USA

Abstract

AbstractAs candidates for intravesical exfoliants to treat bladder cancer, we have prepared fourteen new imidazolium compounds substituted at the 2 position. These compounds were produced by use of the Knoevenagel reaction between a series of aryl aldehydes and 2‐methyl imidazolium salts. Two azolium systems were examined (benzimidazole and 4,5‐dichloroimidazole) and each of these heterocycles are substituted off the nitrogen atom positions with naphthalen‐2‐ylmethyl groups. NMR spectroscopy confirms formation of the carbon‐carbon double bond, and X‐ray crystallography confirmed that the alkenes adopt the E conformation. These new imidazolium salts were evaluated for their chemotherapeutic activity using the NCI‐60 Human Tumor Cell Line Screen, and we observed that the benzimidazolium systems were more toxic than the dichloroimidazolium systems, and that the methyl phenol ether or dimethyl aniline modified compounds showed the highest activities.

Funder

University of Akron

Publisher

Wiley

Reference65 articles.

1. American Cancer Society. Cancer Facts & Figures 2023. Atlanta: American Cancer Society; 2023. .

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