1015792-04-7Relevant articles and documents
Synthesis and structure-activity relationships of harmine derivatives as potential antitumor agents
Cao, Rihui,Fan, Wenxi,Guo, Liang,Ma, Qin,Zhang, Guoxian,Li, Jianru,Chen, Xuemei,Ren, Zhenghua,Qiu, Liqin
, p. 135 - 143 (2013/03/28)
Harmine, a naturally occurring β-carboline alkaloid, showed good antitumor activities together with remarkable neurotoxic effects in animal models. In order to search for novel leading compounds endowed with better antitumor activities and less neurotoxicities, a series of harmine derivatives were designed and synthesized by modification of position-2, 7 and 9 of β-carboline nucleus, and their cytotoxic activities against human tumor cell lines were investigated. Acute toxicities and antitumor activities of the selected compounds in mice were also evaluated. Structure-activity relationships studies confirmed that (1) the 7-methoxy structural moiety was the pharmacophore responsible for the neurotoxic effects of this class of compounds; (2) the substituents in position-2 and 9 played a vital role in modulation of their antitumor activities.
Synthesis and cytotoxic activities of 1-benzylidine substituted β-carboline derivatives
Cao, Rihui,Yi, Wei,Wu, Qifeng,Guan, Xiangdong,Feng, Manxiu,Ma, Chunming,Chen, Zhiyong,Song, Huacan,Peng, Wenlie
scheme or table, p. 6558 - 6561 (2009/09/06)
A series of new β-carboline derivatives, bearing a benzylidine substituent at position-1, has been prepared and evaluated in vitro against a panel of human cell lines. The N2-benzylated β-carbolinium bromates represented the most interesting cytotoxic activities. In particular, compounds 19 were found to be the most potent compounds with IC50 values lower than 5 μM against 10 strains human tumor cell lines. These results confirmed that the N2-benzyl substituent on the β-carboline ring played an important role in the modulation of the cytotoxic activities and suggested that further development of such compounds may be interest.
