40535-46-4Relevant articles and documents
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.
A 9-amino-substituted pyridine and acridine derivatives and its preparation and use
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Paragraph 0009; 0018-0019, (2017/04/13)
The present invention relates to a 9-amino substituted pyrido acridine derivative, a preparation method and uses thereof, wherein the structure formula of the derivative is represented in the instruction. The preparation method comprises that 2-bromobenzoic acid and 8-amino quinoline are adopted to prepare N-(quinolyl)anthranilic acid, the product is subjected to cyclization with phosphorus oxychloride to obtain 9-chloro pyrido acridine, the 9-chloro pyrido acridine is dissolved in ethanol, and benzylamine is added to carry out a nucleophilic substitution reaction so as to prepare the target product. The derivative can be used as an acetylcholinesterase inhibitor so as to be used for the treatment of Alzheimer's disease, cerebrovascular dementia and other diseases.
Acridine derivative, preparation method thereof and application of same serving as anti-tumor drug
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Paragraph 0038; 0040, (2016/12/01)
The invention discloses an acridine derivative and a preparation method and application of the same serving as an anti-tumor drug. The chemical name of the acridine derivative is 7-benzo [b]-[1, 10] phenanthroline p-chlorobenzamide thiourea. The structural formula of the acridine derivative is shown in the description, has the effect of the antitumor activity and has the good application prospect on development of drugs for treating tumors.
