13278-41-6Relevant academic research and scientific papers
Effect of Substituent Size and Isomerization on the Polymorphism of 2-(Naphthalenylamino)-benzoic Acids
Liu, Yuting,Zhang, Mingtao,Xu, Danrui,Parkin, Sean,Li, Tonglei,Li, Conggang,Yang, Zhaoyong,Yu, Faquan,Long, Sihui
, p. 3694 - 3703 (2019)
To probe the effect of substituent size and isomerization on the polymorphism of fenamic acid (FA) derivatives, we synthesized two FA analogues, namely, 2-(naphthalen-1-ylamino)-benzoic acid and 2-(naphthalen-2-ylamino)-benzoic acid (NBAs), and investigat
Design, synthesis, antimicrobial, and anticancer activities of acridine thiosemicarbazides derivatives
Chen, Rui,Huo, Lini,Jaiswal, Yogini,Huang, Jiayong,Zhong, Zhenguo,Zhong, Jing,Williams, Leonard,Xia, Xing,Liang, Yan,Yan, Zhenshuo
, (2019)
Background: Acridine and thiourea derivatives are important compounds in medicinal chemistry due to their diverse biological properties including anticancer and antimicrobial effects. However, literature reveals some side effects associated with use of ac
Discovery of Novel Naphthylphenylketone and Naphthylphenylamine Derivatives as Cell Division Cycle 25B (CDC25B) Phosphatase Inhibitors: Design, Synthesis, Inhibition Mechanism, and in Vitro Efficacy against Melanoma Cell Lines
Cerchia, Carmen,Nasso, Rosarita,Mori, Matteo,Villa, Stefania,Gelain, Arianna,Capasso, Alessandra,Aliotta, Federica,Simonetti, Martina,Rullo, Rosario,Masullo, Mariorosario,De Vendittis, Emmanuele,Ruocco, Maria Rosaria,Lavecchia, Antonio
, p. 7089 - 7110 (2019/08/20)
CDC25 phosphatases play a critical role in the regulation of the cell cycle and thus represent attractive cancer therapeutic targets. We previously discovered the 4-(2-carboxybenzoyl)phthalic acid (NSC28620) as a new CDC25 inhibitor endowed with promising anticancer activity in breast, prostate, and leukemia cells. Herein, we report a structure-based optimization of NSC28620, leading to the identification of a series of novel naphthylphenylketone and naphthylphenylamine derivatives as CDC25B inhibitors. Compounds 7j, 7i, 6e, 7f, and 3 showed higher inhibitory activity than the initial lead, with Ki values in the low micromolar range. Kinetic analysis, intrinsic fluorescence studies, and induced fit docking simulations provided a mechanistic understanding of the activity of these derivatives. All compounds were tested in the highly aggressive human melanoma cell lines A2058 and A375. Compound 4a potently inhibited cell proliferation and colony formation, causing an increase of the G2/M phase and a reduction of the G0/G1 phase of the cell cycle in both cell lines.
7-benz[c]acridine(4-p-fluorophenyl)-1,2,3-triazole as well as preparation method and application thereof
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Paragraph 0025; 0047; 0048, (2016/10/27)
The invention discloses a benz[c]acridine-1,2,3-triazole compound as well as a preparation method and application thereof. The preparation method of the 7-benz[c]acridine-1,2,3-triazole compound comprises the following steps: 1) taking o-bromobenzoic acid
7-p-methoxybenzyl-amino-benzo[c]acridine hydrochloride and preparation method and application thereof
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Paragraph 0029; 0037; 0041; 0042; 0043, (2016/10/10)
The invention discloses 7-p-methoxybenzyl-amino-benzo[c]acridine hydrochloride which has a structural formula as shown in the specification. The 7-p-methoxybenzyl-amino-benzo[c]acridine hydrochloride has high selectivity, has obvious inhibiting effects on
7-benz[c]acridine(4-p-methoxyphenyl)-1,2,3-triazole as well as preparation method and application thereof
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Paragraph 0025, (2016/10/10)
The invention discloses a 7-benz[c]acridine-1,2,3-triazole compound as well as a preparation method and application thereof. The preparation method of the 7-benz[c]acridine-1,2,3-triazole compound comprises the following steps: 1) taking o-bromobenzoic ac
7-benz[c]acridine(4-p-methylphenyl)-1,2,3-triazole and preparation method thereof
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Paragraph 0009; 0025, (2016/10/17)
The invention discloses a benz[c]acridine-1,2,3-triazole compound as well as a preparation method and application thereof. The preparation method of the 7-benz[c]acridine-1,2,3-triazole compound comprises the following steps: 1) taking o-bromobenzoic acid
7-p-toluene aminobenzo [c] acridine hydrochloride and preparation method and application thereof
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Paragraph 0028-0031, (2017/02/09)
The invention discloses 7-p-toluene aminobenzo [c] acridine hydrochloride. The structural formula of the 7-p-toluene aminobenzo [c] acridine hydrochloride is shown in the description, and the 7-p-toluene aminobenzo [c] acridine hydrochloride is high in se
Benzo(c)acridine derivative, and preparation method and use thereof
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Paragraph 0029; 0032, (2016/10/10)
The invention discloses a benzo(c)acridine derivative, and a preparation method and a use thereof. The chemical title of the benzo(c)acridine derivative is 7-benzo(c)acridinylamidothiourea, and the derivative has a structural formula shown in the descript
7-benzo(c)acridine-p-fluorobenzamidothiourea, preparation method and application thereof
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Paragraph 0028; 0031, (2016/12/01)
The invention discloses 7-benzo(c)acridine-p-fluorobenzamidothiourea, a preparation method and an application thereof, wherein the compound has the following structure formula. The invention also provides the application of the compound in preparation of
