Multi-substituted N-phenyl-2, 2-dichloroacetamide analogues as anti-cancer drugs: design, synthesis and biological evaluation

Multi-substituted N-phenyl-2, 2-dichloroacetamide analogues as anti-cancer drugs: design, synthesis and biological evaluation

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 evalua...

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Veröffentlicht in:Yao hsüeh hsüeh pao 2012-03, Vol.47 (3), p.354-363
Hauptverfasser: Li, Tian-Wen, Yang, Yong-Chong, Cheng, Chang-Mei, Wang, Dong-Chun, Lu, Ai-Jun, Zhao, Yu-Fen
Format: Artikel
Sprache:eng
Schlagworte:
Acetamides - chemical synthesis
Acetamides - chemistry
Acetamides - pharmacology
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Apoptosis - drug effects
Carcinoma, Non-Small-Cell Lung - pathology
Cell Line, Tumor
Drug Design
Humans
Inhibitory Concentration 50
Molecular Structure
Structure-Activity Relationship
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Zusammenfassung: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.
ISSN:0513-4870