Mingze Qin

4-Arylindolines Bearing a Pyrido[3,2- d ]pyrimidine Scaffold as Dual Inhibitors of the PD-1/PD-L1 Interaction and NAMPT for Targeting Tumor Immunoevasion and Metabolism

Yangyang Meng, Yuan Yang, Xuejian Wang, Yanqi Jin et autres

Targeting both the PD-1/PD-L1 axis and NAMPT represents a promising therapeutic strategy to overcome resistance to the immune checkpoint blockade. Herein, we developed a novel series of 4-arylindolines bearing a pyrido[3,2- d ]pyrimidine scaffold as dual-targeting inhibitors. Among these, compound B14 emerged …

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Design, synthesis, and biological evaluation of BODIPY-based photoactivatable Crizotinib prodrugs for precision cancer therapy

Chuang Xu, Peiying Lu, Mingze Qin, Ming Ji et autres

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Discovery of Tetrazolone derivatives as potent PPARα/δ dual agonists for metabolic dysfunction-associated steatohepatitis

Yaning Yao, Jiahui Feng, Hao Yue, Jie Wu et autres

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Discovery of potent TNIK inhibitors containing a 1H-pyrrolo[2,3-b]pyridine scaffold as promising therapeutics for colorectal cancer

Xinyu Niu, Shaopeng Zhang, Bing Ying Xu, Wensong Deng et autres

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Discovery of Tetrazolone Derivatives as Potent PPARα/δ Dual Agonists for Metabolic Dysfunction-Associated Steatohepatitis

Yaning Yao, Jiahui Feng, Hao Yue, Jie Wu et autres

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Design, Synthesis, and Biological Evaluation of BODIPY-Based Photoactivatable Crizotinib Prodrugs for Precision Cancer Therapy

Chuang Xu, Peiying Lu, Mingze Qin, Ming Ji et autres

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Novel Isoidide Subunit-Containing Xanthine Oxidase Inhibitors with Potent Hypouricemic Effects

Xiaoyi Zeng, Yu Chen, Jie Zhang, Kun Huang et autres

Abstract Gout is one of the most common inflammatory arthritic diseases. Clinically, the need for safer and more effective xanthine oxidase (XO) inhibitors remains unmet. Here, a novel series of isoidide subunit-containing XO inhibitors was developed through structural optimization of febuxostat. Compounds …

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A combined theoretical and experimental analysis of Vonoprazan fumarate: Crystallographic structure, atropisomerism, molecular docking, dynamics simulation and DFT investigations

Tao Liu, Chengjun Wu, Mingze Qin, Yue Wu et autres

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The Ecological Sensitivity of Traditional Villages Based on Multi-Source Data and Spatial Mechanisms: A Comparative Study of Typical Provinces in China

Xue Jiang, Mingze Qin, Jia Liu, Siqi Wang et autres

Ecological sensitivity provides a critical scientific foundation for enhancing the resilience and sustainable development of traditional villages. However, regional differences in ecological sensitivity remain underexplored. This study investigated the spatial heterogeneity in representative northern (Hebei) and southern (Hubei) Chinese provinces using a …

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Discovery of Pyrazole-Containing 4-Arylindolines as Potent Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction

Yuan Yang, Teng Zhou, Bing Ying Xu, Xiaoyao Zhao et autres

The development of small-molecule inhibitors targeting the programmed cell death-1(PD-1)/programmed cell death-ligand 1 (PD-L1) interaction has emerged as a promising strategy in tumor immunotherapy. In this study, a series of 4-arylindoline derivatives containing a pyrazole moiety were designed and synthesized through a …

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Inverse Agonists of Peroxisome Proliferator-Activated Receptor Gamma: Advances and Prospects in Cancer Treatment

Xuejian Wang, Xinyu Niu, Xiangjie Zhang, Yunlei Hou et autres

Peroxisome proliferator-activated receptor gamma (PPARγ) is a ligand-dependent nuclear transcription factor that modulates metabolic homeostasis and cell proliferation. Inverse agonism of PPARγ is an emerging anticancer strategy, particularly for the treatment of bladder cancer. The first-in-class PPARγ inverse agonist, FX-909, is currently …

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Microscopic damage evolution and physical–mechanical behavior of high-temperature red sandstone under varying heating and cooling durations

Mingze Qin, Yang Su, Xiaolan Wang, Huawei Niu et autres

The investigation into the cooling and heating duration is crucial for evaluating the aftermath of a fire incident. This study comprehensively analyzes the macroscopic and microscopic characteristics of red sandstone under high temperatures, heating, and cooling conditions, with temperatures ranging from 200 …

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