13278-41-6Relevant articles and documents
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
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-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
