1178894-30-8Relevant articles and documents
Synthesis and Evaluation of 3-(Indol-3-yl)-4-(Pyrazolo[3,4-c]Pyridazin-3-yl)-Maleimides as Potent Mutant Isocitrate Dehydrogenase-1 Inhibitors
Xu, Jianghong,Hu, Yuanyuan,Liu, Xiaoqi,Gao, Anhui,Gao, Lixin,Xu, Lei,Zhou, Yubo,Gao, Jianrong,Ye, Qing,Hu, Chunqi,Li, Ji
, p. 655 - 664 (2021/10/25)
A series of new 3-(indol-3-yl)-4-(pyrazolo[3,4-c]pyridazin-3-yl)-maleimides were synthesized and evaluated for their inhibitory activity against IDH1-R132H. Most compounds exhibited significant potency to IDH1-R132H inhibition. Among these, 3-(1-(3-(1H-imidazol-1-yl)propyl)-6-bromo-1H-indol-3-yl)-4-(1-methyl-1H-pyrazolo[3,4-c]pyridazin-3-yl)-1H-pyrrole-2,5-dione (compound IXb), was the most promising IDH1-R132H inhibitor (IC50 = 0.031 μM) and could significantly inhibit the production of 2-HG in U87MG IDH1-R132H cells. Preliminary structure–activity relationships and molecular modeling studies are discussed based on the experimental data obtained.
Synthesis and biological evaluation of 3-chloro-4-(indol-3-yl)-2,5- pyrroledione derivatives as antitumor agents
Lin, Yuchen,Chen, Jing
, p. 382 - 389 (2013/07/26)
A series of 3-chloro-4-(indol-3-yl)-2,5-pyrroledione derivatives were synthesized and evaluated for their cytotoxic activities in vitro against five human cancer cell lines (K562, A549, ECA-109, KB and SMMC-7721). Most compounds displayed potent cytotoxicity with IC50 values in low micromolar range. The results showed that the existence of the chlorine atom at 3-position on the pyrroledione ring was crucial for the activity. Compound 6a, the most potent one (IC50: 0.67~3.93 μM), would be a promising template for further development of novel antitumor agents.