Related Experiment Video
Updated: Jul 15, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Novel potent antimitotic heterocyclic ketones: synthesis, antiproliferative activity, and structure-activity
Laixing Hu1, Jian-dong Jiang, Jinrong Qu
1Department of Chemistry, Georgia State University, Atlanta, GA 30303-3083, USA.
Abstract:
We report the synthesis, antiproliferative activity, and SAR of novel heterocyclic ketones derived from carbazole sulfonamides. Most of the heterocyclic ketones showed strong cytotoxicities. (N-1-Methylindole-5-yl)-(3,4,5-trimethoxyphenyl)-methanone 8b gave the most potent cytotoxicity (9.2-26 nM) against seven human tumor cell lines. The mechanism of action of the heterocyclic ketones appears to involve targeting of tubulin, similar to that of CA-4 and different from the carbazole sulfonamides.
Related Concept Videos
Antiviral Nucleoside Inhibitors
Inhibition of Cdk Activity
Inhibition of CDK Activity
Antifungal Agents
Local Anesthetics: Chemistry and Structure-Activity Relationship
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
