Synthesis and structure-activity relationship of N-(2-arylethyl) isoquinoline derivatives as anti-cancer agents.
- Author:
Yan-Xiang WANG
1
;
Wu-Li ZHAO
;
Chong-Wen BI
;
Yang-Biao LI
;
Rong-Guang SHAO
;
Dan-Qing SONG
Author Information
1. Institute of Medicinal Biotechnology, China Academy of Medical Science and Peking Union Medical College, Beijing 100050, China.
- Publication Type:Journal Article
- MeSH:
Antineoplastic Agents;
chemical synthesis;
chemistry;
pharmacology;
Cell Cycle;
drug effects;
Cell Proliferation;
drug effects;
HCT116 Cells;
Hep G2 Cells;
Humans;
Inhibitory Concentration 50;
Isoquinolines;
chemical synthesis;
chemistry;
pharmacology;
Molecular Structure;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2012;47(2):200-205
- CountryChina
- Language:Chinese
-
Abstract:
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.
