Synthesis and cytotoxic activities of 1-benzylidine substituted beta-carboline derivatives |
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Authors: | Cao Rihui Yi Wei Wu Qifeng Guan Xiangdong Feng Manxiu Ma Chunming Chen Zhiyong Song Huacan Peng Wenlie |
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Institution: | School of Chemistry and Chemical Engineering, Sun Yat-sen (Zhongshan) University, 135 Xin Gang Xi Road, Guangzhou 510275, PR China. caorihui@mail.sysu.edu.cn |
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Abstract: | A series of new beta-carboline derivatives, bearing a benzylidine substituent at position-1, has been prepared and evaluated in vitro against a panel of human cell lines. The N(2)-benzylated beta-carbolinium bromates represented the most interesting cytotoxic activities. In particular, compounds 19 were found to be the most potent compounds with IC(50) values lower than 5 microM against 10 strains human tumor cell lines. These results confirmed that the N(2)-benzyl substituent on the beta-carboline ring played an important role in the modulation of the cytotoxic activities and suggested that further development of such compounds may be interest. |
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