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Updated: May 6, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
[Synthesis and biological evaluation of diarylamines with antitumor activity]
Sheng-Biao Wang1, Xiao-Feng Wang, Lan Xie
1College of Pharmaceutical Sciences, Central South University, Changsha 410013, China.
Abstract:
By structural modifications of our previous leads 1-3, 18 diarylamines were designed, synthesized and evaluated with a human tumor cell line panel, including A549, DU145, KB, and KB-vin cell lines, resulting in the discovery of new antitumor agents A6 and B2 with low micromolar G50 values ranging from 1.55-2.10 micromol x L(-1) for above cell lines, and A9 with GI50 values ranging from 1.55-2.10 micromol x L(-1) specially for DU145, KB, and KB-vin cells. Current structure-activity relationships are helpful for further lead optimization.
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