1380693-71-9Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of β-carboline 1,3,4-oxadiazole based hybrids as HDAC inhibitors with potential antitumor effects
Tian, Caizhi,Huang, Shuoqi,Xu, Zihua,Liu, Wenwu,Li, Deping,Liu, Mingyue,Zhu, Chengze,Wu, Limeng,Jiang, Xiaowen,Ding, Huaiwei,Zhao, Qingchun
, (2022/03/23)
A series of novel β-carboline 1,3,4-oxadiazole based hybrids were designed, synthesized, and tested for cytotoxicity and HDAC inhibition. Among the target compounds, compound ZDLT-1 displayed high inhibitory activity for class I HDACs 1, 2, and 3, and potent anti-proliferative activity against HCT116 cells with an IC50 value of 0.173 ± 0.018 μM, it also exhibited better inhibitory activity with an IC50 value of 6 nM for HDAC6 than SAHA (IC50 = 15 nM). Furthermore, the pharmacological experiment of Hoechst staining, colony formation, cell apoptosis assay, and wound healing scratch assay indicated that compound ZDLT-1 was a potent cytotoxic agent against HCT116 cells with cell apoptosis induction. Further, in silico prediction of physicochemical properties, drug-likeness, and ADME parameters suggested that compound ZDLT-1 is a promising anticancer agent. Taken together, the high potency cytotoxicity and class I HDACs inhibitory activity of compound ZDLT-1, which with the β-carboline 1,3,4-oxadiazole based hybrids as potent anticancer agents could be nominated for further modification and optimization.
Synthesis and herbicidal activity evaluation of novel β-carboline derivatives
Weng, Qunfang,Huang, Jingfei,Zeng, Yong,Deng, Yueye,Hu, Meiying
, p. 3969 - 3980 (2012/09/10)
Based on the original structure of harmine, several novel 1,2,3,4-tetrahydro-β- carboline, β-carboline and 1-substituted-β- carboline derivatives bearing a substituted carbohydrazide group at C-3 were designed and synthesized to investigate the structureactivity relationship of their analogues. All of the compounds were characterized by infrared (IR), proton and carbon nuclear magnetic resonance (1H-NMR, 13C-NMR), and mass spectroscopy (MS). The bioassay tests showed that N'-benzylidene-1-phenyl-β- carboline-3-carbohydrazide (C25H 18N4O, m.w. 390.4) (c2) and N'-(4- trifluoromethylbenzylidene)- 1-phenyl-β-carboline-3-carbohydrazide (C26H17N4OF3, m.w. 458) (d2) exhibited good inhibitory activity against dicotyledonous and monocotyledonous weeds, with EC50 values of 4.83 μM and 14.25 μM, respectively.
