752212-92-3Relevant articles and documents
Design, synthesis, and biological evaluation of novel N-acylhydrazone bond linked heterobivalent β-carbolines as potential anticancer agents
Chen, Xiaofei,Guo, Liang,Ma, Qin,Chen, Wei,Fan, Wenxi,Zhang, Jie
, (2019/08/22)
Utilizing a pharmacophore hybridization approach, we have designed and synthesized a novel series of 28 new heterobivalent β-carbolines. The in vitro cytotoxic potential of each compound was evaluated against the five cancer cell lines (LLC, BGC-823, CT-26, Bel-7402, and MCF-7) of different origin—murine and human, with the aim of determining the potency and selectivity of the compounds. Compound 8z showed antitumor activities with half-maximal inhibitory concentration (IC50) values of 9.9 ± 0.9, 8.6 ± 1.4, 6.2 ± 2.5, 9.9 ± 0.5, and 5.7 ± 1.2 μM against the tested five cancer cell lines. Moreover, the effect of compound 8z on the angiogenesis process was investigated using a chicken chorioallantoic membrane (CAM) in vivo model. At a concentration of 5 μM, compound 8z showed a positive effect on angiogenesis. The results of this study contribute to the further elucidation of the biological regulatory role of heterobivalent β-carbolines and provide helpful information on the development of vascular targeting antitumor drugs.
Synthesis, acute toxicities, and antitumor effects of novel 9-substituted β-carboline derivatives
Cao, Rihui,Chen, Qi,Hou, Xuerui,Chen, Hongsheng,Guan, Huaji,Ma, Yan,Peng, Wenlie,Xu, Anlong
, p. 4613 - 4623 (2007/10/03)
A series of novel 9-substituted β-carboline derivatives was synthesized from the starting material harmine and l-tryptophan, respectively. Cytotoxic activities, acute toxicities, and antitumor effects of these compounds were investigated. A series of nove
