Synthesis and biological evaluation of diarylamines with antitumor activity.
- Author:
Sheng-Biao WANG
1
;
Xiao-Feng WANG
;
Lan XIE
Author Information
1. College of Pharmaceutical Sciences, Central South University, Changsha 410013, China.
- Publication Type:Journal Article
- MeSH:
Amines;
chemical synthesis;
chemistry;
pharmacology;
Antineoplastic Agents;
chemical synthesis;
chemistry;
pharmacology;
Cell Line, Tumor;
Cell Proliferation;
drug effects;
Drug Design;
Drug Screening Assays, Antitumor;
Humans;
Molecular Structure;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2013;48(8):1273-1280
- CountryChina
- Language:Chinese
-
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.
