Synthesis and structure-activity relationship of N-(2-arylethyl) isoquinoline derivatives as anti-cancer agents

Synthesis and structure-activity relationship of N-(2-arylethyl) isoquinoline derivatives as anti-cancer agents

A series of novel N-(2-arylethyl) isoquinoline derivatives were designed, synthesized and evaluated for their anti-cancer activities. Among these analogs, compound 9a exhibited the potential anti-cancer activities on HepG2 and HCT116 cells with IC50 values of 2.52 and 1.99 microg x mL(-1), respectiv...

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Veröffentlicht in:Yao hsüeh hsüeh pao 2012-02, Vol.47 (2), p.200-205
Hauptverfasser: Wang, Yan-Xiang, Zhao, Wu-Li, Bi, Chong-Wen, Li, Yang-Biao, Shao, Rong-Guang, Song, Dan-Qing
Format: Artikel
Sprache:chi
Schlagworte:
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Cell Cycle - drug effects
Cell Proliferation - drug effects
HCT116 Cells
Hep G2 Cells
Humans
Inhibitory Concentration 50
Isoquinolines - chemical synthesis
Isoquinolines - chemistry
Isoquinolines - pharmacology
Molecular Structure
Structure-Activity Relationship
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Zusammenfassung:A series of novel N-(2-arylethyl) isoquinoline derivatives were designed, synthesized and evaluated for their anti-cancer activities. Among these analogs, compound 9a exhibited the potential anti-cancer activities on HepG2 and HCT116 cells with IC50 values of 2.52 and 1.99 microg x mL(-1), respectively. Cell cycle was blocked at S phase of HepG2 cells treated with 9a by flow cytometry detection. Our results provided a basis for the development of a new series of anti-cancer candidates.
ISSN:0513-4870