27696-24-8Relevant articles and documents
Tricyclic heterocycles display diverse sensitivity to the A147T TSPO polymorphism
Sokias, Renee,Werry, Eryn L.,Alison Cheng, Hei Wun,Lloyd, James H.,Sohler, Greta,Danon, Jonathan J.,Montgomery, Andrew P.,Du, Jonathan J.,Gao, Quanqing,Hibbs, David E.,Ittner, Lars M.,Reekie, Tristan A.,Kassiou, Michael
, (2020)
The 18 kDa translocator protein (TSPO) is a target for the development of imaging agents to detect neuroinflammation. The clinical utility of second-generation TSPO ligands has been hindered by the presence of a polymorphism, rs6971, which causes a non-co
Design, synthesis, antitumor evaluation, 3D-QSAR and molecular docking studies of novel 4-aminoacridone compounds
Tian, Lin,Feng, Chang J.,Li, Tong X.,Li, Zhao,Yang, Wei H.,Han, Xiang E.
, p. 2538 - 2546 (2017)
4-aminoacridone was efficiently synthesized using an optimized method and condensed with a variety of different aldehydes to give the corresponding Schiff bases, 1a–k. The antiproliferative activities of these compounds were measured against several human
Synthesis of 11-(Piperazin-1-yl)-5H-dibenzo[b,e] [1,4]diazepine on kilo scale
Kalhapure, Rahul S.,Patil, Bhushan P.,Jadhav, Mahantesh N.,Kawle, Laxmikant A.,Wagh, Sanjay B.
, p. 1747 - 1749 (2011)
A synthesis of 11-(piperazin-1yl)-5H-dibenzo[b,e][1,4]diazepine on kilo scale without any chromatographic purification step is reported. Key steps involved are Ullmann condensation, catalytic hydrogenation, and catalyzed cyclization. Copyright E-Journal o
Design, synthesis and biological evaluation of N-anthraniloyl tryptamine derivatives as pleiotropic molecules for the therapy of malignant glioma
Fan, Xiaohong,Li, Junfang,Long, Lin,Shi, Tao,Liu, Dan,Tan, Wen,Zhang, Honghua,Wu, Xiaoyan,Lei, Xiaoyong,Wang, Zhen
, (2021/06/09)
COX-2 and STAT3 are two key culprits in the glioma microenvironment. Herein, to inhibit COX-2 and block STAT3 signaling, we disclosed 27 N-anthraniloyl tryptamine compounds based on the combination of melatonin derivatives and N-substituted anthranilic acid derivatives. Among them, NP16 showed the best antiproliferative activity and moderate COX-2 inhibition. Of note, NP16 decreased the level of p-JAK2 and p-STAT3, and blocked the nuclear translocation of STAT3 in GBM cell lines. Moreover, NP16 downregulated the MMP-9 expression of BV2 cells in a co-culture system of BV2 and C6 glioma cells, abrogated the proliferative/invasive/migratory abilities of GBM cells, induced apoptosis by ROS and the Bcl-2-regulated apoptotic pathway, and induced obvious G2/M arrest in glioma cells in vitro. Furthermore, NP16 displayed favorable pharmacokinetic profiles covering long half-life (11.43 ± 0.43 h) and high blood-brain barrier permeability. Finally, NP16 effectively inhibited tumor growth, promoted the survival rate, increased the expression of E-cadherin and reduced overproduction of PGE2, MMP-9, VEGF-A and the level of p-STAT3 in tumor tissue, and improved the anxiety-like behavior in C6 glioma model. All these evidences demonstrated N-anthraniloyl tryptamine derivatives as multifunctional anti-glioma agents with high potency could drain the swamp to beat glioma.
