220407-33-0Relevant articles and documents
3-(7-Azaindolyl)-4-indolylmaleimides as a novel class of mutant isocitrate dehydrogenase-1 inhibitors: Design, synthesis, and biological evaluation
Hu, Yuanyuan,Gao, Anhui,Liao, Honghui,Zhang, Mengmeng,Xu, Gaoya,Gao, Lixin,Xu, Lei,Zhou, Yubo,Gao, Jianrong,Ye, Qing,Li, Jia
, (2018/09/06)
A series of 3-(7-azainodyl)-4-indolylmaleimides was designed, synthesized, and evaluated for their isocitrate dehydrogenase 1 (IDH1)/R132H inhibitory activities. Many compounds such as 11a, 11c, 11e, 11g, and 11s exhibited favorable inhibitory effects on IDH1/R132H and were highly selective against the wild-type IDH1. Evaluation of the biological activities at the cellular level showed that compounds 11a, 11c, 11e, 11g, and 11s could effectively suppress the production of 2-hydroxyglutaric acid in U87MG cells expressing IDH1/R132H. Preliminary structure–activity relationship (SAR) and molecular modeling studies were discussed based on the experimental data obtained. These findings may provide new insights into the development of novel IDH1/R132H inhibitors.
3 - (1, 2, 4 - triazole [4, 3 - a] pyridine - 3 - yl) - 4 - (1H - Indol - 3 - yl) maleimide derivatives and its preparation method and application
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Paragraph 0035; 0036; 0049; 0050, (2017/08/25)
The invention provides a 3-(1,2,4-triazolo(4,3-a)pyridine-3-yl)-4-(1H-indole-3-yl)maleimide derivative with a novel structure and a preparation method and application of the derivative. The compound can be used for treating ischemic cerebral apoplexy. The general structural formula of the compound is shown in the specification.
Synthesis and Evaluation of 3-(furo[2,3-b]pyridin-3-yl)-4-(1H-indol-3-yl)-maleimides as Novel GSK-3β Inhibitors and Anti-Ischemic Agents
Ye, Qing,Li, Qiu,Zhou, Yubo,Xu, Lei,Mao, Weili,Gao, Yuanxue,Li, Chenhui,Xu, Yuan,Xu, Yazhou,Liao, Hong,Zhang, Luyong,Gao, Jianrong,Li, Jia,Pang, Tao
, p. 746 - 752 (2015/03/30)
A series of novel 3-(furo[2,3-b]pyridin-3-yl)-4-(1H-indol-3-yl)-maleimides were designed, synthesized, and biologically evaluated for their GSK-3β inhibitory activities. Most compounds showed favorable inhibitory activities against GSK-3β protein. Among them, compounds 5n, 5o, and 5p significantly reduced GSK-3β substrate tau phosphorylation at Ser396 in primary neurons, indicating inhibition of cellular GSK-3β activity. In the in vitro neuronal injury models, compounds 5n, 5o, and 5p prevented neuronal death against glutamate, oxygen-glucose deprivation, and nutrient serum deprivation which are closely associated with cerebral ischemic stroke. In the in vivo cerebral ischemia animal model, compound 5o reduced infarct size by 10% and improved the neurological deficit. The results may provide new insights into the development of novel GSK-3β inhibitors with potential neuroprotective activity against brain ischemic stroke.
Synthesis and biological evaluation of 3-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-4-(indol-3-yl)-maleimides as potent, selective GSK-3β inhibitors and neuroprotective agents
Ye, Qing,Mao, Weili,Zhou, Yubo,Xu, Lei,Li, Qiu,Gao, Yuanxue,Wang, Jing,Li, Chenhui,Xu, Yazhou,Xu, Yuan,Liao, Hong,Zhang, Luyong,Gao, Jianrong,Li, Jia,Pang, Tao
, p. 1179 - 1188 (2015/03/04)
A series of novel 3-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-4-(indol-3-yl)-maleimides were designed, prepared and evaluated for their GSK-3β inhibitory activities. Most compounds showed high potency to GSK-3β inhibition with high selectivity. Among them, compounds 7c, 7f, 7h, 7l and 7m significantly reduced GSK-3β substrate Tau phosphorylation at Ser396 in primary neurons, showing the inhibition of cellular GSK-3β. In the in vitro neuronal injury models, compounds 7c, 7f, 7h, 7l and 7m prevented neuronal death against glutamate, oxygen-glucose deprivation and nutrient serum deprivation which are associated with cerebral ischemic stroke. In the in vivo cerebral ischemia animal model, compound 7f reduced infarct size by 15% and improved the neurological deficit following focal cerebral ischemia. These findings may provide new insights into the development of novel GSK-3β inhibitors with potential neuroprotective activity.
Synthesis and biological evaluation of 3-benzisoxazolyl-4-indolylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3β
Ye, Qing,Li, Meng,Zhou, Yubo,Pang, Tao,Xu, Lei,Cao, Jiayi,Han, Liang,Li, Yujin,Wang, Weisi,Gao, Jianrong,Li, Jia
, p. 5498 - 5516 (2013/06/27)
A series of novel 3-benzisoxazolyl-4-indolyl-maleimides were synthesized and evaluated for their GSK-3β inhibitory activity. Most compounds exhibited high inhibitory potency towards GSK-3β. Among them, compound 7j with an IC50 value of 0.73 nM was the most promising GSK-3β inhibitor. Preliminary structure-activity relationships were examined and showed that different substituents on the indole ring and N1-position of the indole ring had varying degrees of influence on the GSK-3β inhibitory potency. Compounds 7c, 7f, 7j-l and 7o-q could obviously reduce Aβ-induced Tau hyperphosphorylation by inhibiting GSK-3β in a cell-based functional assay.
Design, synthesis, and evaluation of 3-aryl-4-pyrrolyl-maleimides as glycogen synthase kinase-3β inhibitors
Ye, Qing,Li, Meng,Zhou, Yu-Bo,Cao, Jia-Yu,Xu, Lei,Li, Yu-Jin,Han, Liang,Gao, Jian-Rong,Hu, Yong-Zhou,Li, Jia
, p. 349 - 358 (2013/07/19)
A series of 3-aryl-4-pyrrolyl-maleimides were designed, synthesized, and evaluated for their glycogen synthase kinase-3β (GSK-3β) inhibitory activity. Most compounds exhibited potent activity against GSK-3β. Among them, compounds 11a, 11c, 11h, 11i, and 11j significantly reduced Aβ-induced Tau hyperphosphorylation, showing the inhibition of GSK-3β at the cellular level. Structure-activity relationships were discussed based on the experimental data obtained. Most compounds in a new series of 3-aryl-4-pyrrolyl-maleimides exhibited potent glycogen synthase kinase-3β (GSK-3β) inhibitory activity. Compounds 11a, 11c, 11h, 11i, and 11j reduced Aβ-induced Tau hyperphosphorylation, showing inhibition of GSK-3β at the cellular level. Copyright
Total Synthesis of (±)-Perophoramidine
Fuchs, James R.,Funk, Raymond L.
, p. 5068 - 5069 (2007/10/03)
The first total synthesis of racemic perophoramidine is described. The key step features the highly stereoselective introduction of the vicinial quaternary centers via base-promoted carbon-carbon bond formation between a 3-alkylindole and a 3-bromo-3-alkylindolin-2-one. This transformation presumably proceeds through a conjugate addition or Diels-Alder cycloaddition of the 3-alkylindole with a 3-alkylindol-2-one intermediate. Copyright
Novel, potent and selective cyclin D1/CDK4 inhibitors: Indolo[6,7-a]pyrrolo[3,4-c]carbazoles
Engler, Thomas A.,Furness, Kelly,Malhotra, Sushant,Sanchez-Martinez, Concha,Shih, Chuan,Xie, Walter,Zhu, Guoxin,Zhou, Xun,Conner, Scott,Faul, Margaret M.,Sullivan, Kevin A.,Kolis, Stanley P.,Brooks, Harold B.,Patel, Bharvin,Schultz, Richard M.,DeHahn, Tammy B.,Kirmani, Kashif,Spencer, Charles D.,Watkins, Scott A.,Considine, Eileen L.,Dempsey, Jack A.,Ogg, Catherine A.,Stamm, Nancy B.,Anderson, Bryan D.,Campbell, Robert M.,Vasudevan, Vasu,Lytle, Michelle L.
, p. 2261 - 2267 (2007/10/03)
The synthesis and CDK inhibitory properties of a series of indolo[6,7-a]pyrrolo[3,4-c]carbazoles is reported. In addition to their potent CDK activity, the compounds display antiproliferative activity against two human cancer cell lines. These inhibitors also effect strong G1 arrest in these cell lines and inhibit Rb phosphorylation at Ser780 consistent with inhibition of cyclin D1/CDK4.
Total synthesis of didemnimide A and B
Hughes, Terry V.,Cava, Michael P.
, p. 9629 - 9630 (2007/10/03)
The total synthesis of didemnimide A and didemnimide B, novel predator- deterrent alkaloids from the Caribbean mangrove ascidian Didemnum conchyliatum, is described.
