Multi-substituted N-phenyl-2, 2-dichloroacetamide analogues as anti-cancer drugs: design, synthesis and biological evaluation.
- Author:
Tian-Wen LI
1
;
Yong-Chong YANG
;
Chang-Mei CHENG
;
Dong-Chun WANG
;
Ai-Jun LU
;
Yu-Fen ZHAO
Author Information
1. Key Laboratory of Bioorganic Phosphorus and Chemical Biology, Ministry of Education, Department of Chemistry, Tsinghua University, Beijing 100084, China.
- Publication Type:Journal Article
- MeSH:
Acetamides;
chemical synthesis;
chemistry;
pharmacology;
Antineoplastic Agents;
chemical synthesis;
chemistry;
pharmacology;
Apoptosis;
drug effects;
Carcinoma, Non-Small-Cell Lung;
pathology;
Cell Line, Tumor;
Drug Design;
Humans;
Inhibitory Concentration 50;
Molecular Structure;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2012;47(3):354-363
- CountryChina
- Language:English
-
Abstract:
Our earlier research has shown that mono-substituted N-phenyl-2, 2-dichloroacetamide exhibited much higher anti-cancer activity than the lead compound sodium dichloroacetate (DCA). In this paper, a variety of multi-substituted N-phenyl-2, 2-dichloroacetamides were synthesized and biologically evaluated. The results showed that 3, 5-disubstituted N-phenyl-2, 2-dichloroacetamide analogues had satisfactory potency. Among them, N-(3, 5-diiodophenyl)-2, 2-dichloroacetamide had an IC50 of 2.84 micromol x L(-1) against non-small cell lung cancer cell line A549 and could induce cancer cell apoptosis.
