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fold decrease » fold increase (Expand Search), fold increased (Expand Search)
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50 c » 5 c (Expand Search), 50 μ (Expand Search), 50 _ (Expand Search)
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Design of Benzyl-triazolopyrimidine-Based NADPH Oxidase Inhibitors Leads to the Discovery of a Potent Dual Covalent NOX2/MAOB Inhibitor
Published 2025“…We found that <b>9a</b>, bearing a pargyline moiety, is also able to selectively inhibit MAOB over MAOA (465-fold) with an IC<sub>50</sub> of 0.182 μM, being the first-in-class dual NOX2/MAOB covalent inhibitor. …”
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168
Development of (2-(Benzyloxy)phenyl)methanamine Derivatives as Potent and Selective Inhibitors of CARM1 for the Treatment of Melanoma
Published 2024“…In our previous study, we have identified a series of type I PRMT inhibitors, among which ZL-28-6 (<b>6</b>) exhibited increased activity against CARM1 while displaying decreased potency against other type I PRMTs. …”
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169
Development of (2-(Benzyloxy)phenyl)methanamine Derivatives as Potent and Selective Inhibitors of CARM1 for the Treatment of Melanoma
Published 2024“…In our previous study, we have identified a series of type I PRMT inhibitors, among which ZL-28-6 (<b>6</b>) exhibited increased activity against CARM1 while displaying decreased potency against other type I PRMTs. …”
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170
Development of (2-(Benzyloxy)phenyl)methanamine Derivatives as Potent and Selective Inhibitors of CARM1 for the Treatment of Melanoma
Published 2024“…In our previous study, we have identified a series of type I PRMT inhibitors, among which ZL-28-6 (<b>6</b>) exhibited increased activity against CARM1 while displaying decreased potency against other type I PRMTs. …”
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171
First-in-Class Hydrazide-Based HDAC6 Selective Inhibitor with Potent Oral Anti-Inflammatory Activity by Attenuating NLRP3 Inflammasome Activation
Published 2022“…In this study, we report the first highly selective HDAC6 inhibitor with hydrazide as the zinc-binding group (ZBG), which displays superior pharmacokinetic properties to the current hydroxamic acid inhibitors. …”
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172
First-in-Class Hydrazide-Based HDAC6 Selective Inhibitor with Potent Oral Anti-Inflammatory Activity by Attenuating NLRP3 Inflammasome Activation
Published 2022“…In this study, we report the first highly selective HDAC6 inhibitor with hydrazide as the zinc-binding group (ZBG), which displays superior pharmacokinetic properties to the current hydroxamic acid inhibitors. …”
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Discovery of Triazolyl Derivatives of Cucurbitacin B Targeting IGF2BP1 against Non-Small Cell Lung Cancer
Published 2023“…Cucurbitacin B (CuB) is a potent but toxic anticancer natural product. Herein, we designed and synthesized 2-OH- and 16-OH-modified CuB derivatives to improve their antitumor efficacy and reduce toxicity. …”
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2‑Aminobenzoxazole Derivatives as Potent Inhibitors of the Sphingosine-1-Phosphate Transporter Spinster Homolog 2 (Spns2)
Published 2023“…To develop more potent compounds, we initiated a structure–activity relationship study that identified 2-aminobenzoxazole as a viable scaffold. …”
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Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MAGL) Inhibitors: Bioisosteric Transformation from 3‑Oxo-3,4-dihydro‑2<i>H</i>‑ben...
Published 2021“…Optimization of the left hand side afforded <b>4f</b> as a promising reversible MAGL inhibitor, which showed potent in vitro MAGL inhibitory activity (IC<sub>50</sub> 6.2 nM), good oral absorption, blood–brain barrier penetration, and significant pharmacodynamic changes (2-arachidonoylglycerol increase and arachidonic acid decrease) at 0.3–10 mg/kg, po. in mice.…”
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