1145668-27-4Relevant academic research and scientific papers
Synthesis and biological evaluation of piperazine group-linked bivalent β-carbolines as potential antitumor agents
Sun, Rongqin,Liu, Rui,Zhou, Chi,Ren, Zhenghua,Guo, Liang,Ma, Qin,Fan, Wenxi,Qiu, Liqin,Yu, Huijuan,Shao, Guang,Cao, Rihui
, p. 2170 - 2174 (2015/12/11)
A series of novel bivalent β-carbolines with a piperazine group spacer between 3-methylene units were synthesized and evaluated as antitumor agents. The results demonstrated that compounds 7e and 7g exhibited the most potent cytotoxic activities against ten tumor cell lines. Structure-activity relationships analysis indicated that (1) the substituents in positions 1 and 9 of the β-carboline ring played a significant role in modulating the antitumor activity; (2) the introduction of alkyl groups into position-9 of the β-carboline nucleus enhanced their cytotoxic potencies and the butyl substituent was the optimal group. Investigation of the preliminary mechanism of action demonstrated that compound 7g showed obvious anti-angiogenic activity in the in vivo CAM assay, and the potency was similar to that of CA4P (200 μM).
Synthesis and in vitro cytotoxic evaluation of novel 3,4,5-trimethoxyphenyl substituted β-carboline derivatives
Wu, Qifeng,Cao, Rihui,Feng, Manxiu,Guan, Xiangdong,Ma, Chunming,Liu, Jinbing,Song, Huacan,Peng, Wenlie
experimental part, p. 533 - 540 (2009/09/08)
To elucidate further our SARs' study on the chemistry and cytotoxic activity and probe the structural requirement for the potent antitumor activity of β-carbolines, a series of novel 1,9-disubstituted and 1,3,9-trisubstituted β-carboline derivatives were
