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.
7-benzo[b]-[1,10]o-phenanthroline pyridine carboxamide thiourea as well as preparation method and application thereof
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Paragraph 0010; 0021; 0023, (2016/10/27)
The invention discloses 7-benzo[b]-[1,10]o-phenanthroline pyridine carboxamide thiourea as well as a preparation method and application thereof. The structural form is shown in the specification; the 7-site of the benzo[b]-[1,10]o-phenanthroline ring is connected with an active group acylaminothiourea structure to synthesize a novel acridine derivative which has extremely strong antitumor activity and can be applied to the preparation of antitumor drugs.
7-benzo [b] - [1,10] O-phenanthroline the methoxylphenylboronic a amido-thiourea and its preparation and use (by machine translation)
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Paragraph 0024, (2017/01/09)
The invention discloses a 7-benzo [b] - [1,10] O-phenanthroline the methoxylphenylboronic a amido-thiourea and its preparation and use, its structural formula is: The benzo [b] - [1,10] phenanthroline ring adjacent the 7-position is connected with the act
