40535-46-4Relevant academic research and scientific papers
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.
HETEROCYCLIC COMPOUND AND ORGANIC LIGHT EMITTING ELEMENT USING SAME
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Paragraph 0126; 0127; 0128, (2019/09/06)
The present application relates to a hetero-cyclic compound represented by Chemical Formula 1, and an organic light emitting device comprising the same.
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.
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.
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
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.
Synthesis and cytotoxic activity of benzophenanthrolinone analogues of acronycine
Bongui,Elomri,Seguin,Tillequin,Pfeiffer,Renard,Pierre,Atassi
, p. 1077 - 1080 (2007/10/03)
Condensation of either 2-bromobenzoic acid (4) or 2-chloro-3-nitrobenzoic acid (5) with suitable amino-quinolines 6 - 8 afforded phenylquinolylamines 9 - 13. Acid mediated cyclizafion gave the corresponding 12H-benzo[b][1,7]phenanthrolin-7-ones 14 and 15, and 12H-benzo[b][1,10]phenanthrolin-7-ones 16 - 18. Compounds 14, 16, and 17 were subsequently N-methylated to 6-demethoxyacronycine and acronycine analogues 19 - 21, whereas reduction of the aromatic nitro group of 18 gave the amino derivative 22. Unsubstituted 12H-benzo[b][1,10]phenanthrolin-7-ones 16, 17, 20, and 21 were devoid of significant cytotoxic activity, whereas 18 and 22, bearing a nitrogen substituent at position 11, were significantly active. Unsubstituted 12H-benzo[b][1,7]phenanthrolin-7-ones 14 and 19, which include a pyridine nitrogen in the same 4-position as the pyran oxygen of acronycine exhibited cytotoxic activities within the same range of magnitude as acronycine itself.
1,10[8,9-Benz]phenanthroline
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, (2008/06/13)
Compounds represented by the general formula (I) STR1 in which R represents an aniline substituted in the para position by either --NHSO2 CH3 or --NHCOOCH3 and bearing either an --H or --OCH3 in the ortho positi
