Novel Carbamate-Based o-aminobenzamide Derivatives as Potent Antigastric Carcinoma Agents via Disrupting NAD+ Salvage Synthesis
文献类型：期刊论文
| 作者 | Zhang, Siyi; Li, Zhen; Li, Bo; Li, Zhiyi; Peng, Huiqian; Shen, Lixian; Zhu, Lejing; Mo, Tong; Peng, Jialiang; Zhuo, Linsheng |
| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2025 |
| 卷号 | 68期号:11页码:10738 |
| 英文摘要 | Blocking NAD+ biosynthesis presents an appealing strategy for antitumor therapies. This study developed a series of o-aminobenzamide derivatives with substantial antitumor efficacy against gastric cancer. Notably, compound 9a demonstrated exceptional antitumor activity against undifferentiated gastric cancer HGC27 cells (IC50 = 0.049 mu M), and significant inhibitory effects on cellular proliferation, self-renewal, invasion, and migration. Mechanistic investigations revealed that 9a could damage mitochondria, arrest the cell cycle, promote apoptosis, and alter cellular metabolism. Furthermore, the rate-limiting enzyme NAMPT in the NAD+ salvage synthetic pathway was identified as a primary target of 9a. By inhibiting NAMPT, 9a reduced intracellular levels of NAD+ and ATP, while NMN, a natural product of NAMPT, counteracts its antimetabolic and cytotoxic effects. Overall, this study highlights 9a as a promising NAMPT inhibitor with significant activity against undifferentiated gastric cancer, laying the groundwork for developing novel antigastric cancer agents through inhibiting NAD+ biosynthesis. |
| 源URL | [http://210.75.249.4/handle/363003/62435]  |
| 专题 | 西北高原生物研究所_中国科学院西北高原生物研究所 |
| 推荐引用方式 GB/T 7714 | Zhang, Siyi,Li, Zhen,Li, Bo,et al. Novel Carbamate-Based o-aminobenzamide Derivatives as Potent Antigastric Carcinoma Agents via Disrupting NAD+ Salvage Synthesis[J]. JOURNAL OF MEDICINAL CHEMISTRY,2025,68(11):10738. |
| APA | Zhang, Siyi.,Li, Zhen.,Li, Bo.,Li, Zhiyi.,Peng, Huiqian.,...&Jiang, Weifan.(2025).Novel Carbamate-Based o-aminobenzamide Derivatives as Potent Antigastric Carcinoma Agents via Disrupting NAD+ Salvage Synthesis.JOURNAL OF MEDICINAL CHEMISTRY,68(11),10738. |
| MLA | Zhang, Siyi,et al."Novel Carbamate-Based o-aminobenzamide Derivatives as Potent Antigastric Carcinoma Agents via Disrupting NAD+ Salvage Synthesis".JOURNAL OF MEDICINAL CHEMISTRY 68.11(2025):10738. |
入库方式： OAI收割
来源：西北高原生物研究所
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