The synthesis and biological evaluation of novel deuterated and non-deuterated aminobenzenesulfonamide derivatives as EGFR inhibitor [0.03%]
一类新型茋类衍生物的合成及其EGFR抑制活性研究
Puzhuang Hou,Haitao Zhi,Longcai Cao et al.
Puzhuang Hou et al.
Twenty novel pyrimidine derivatives of deuterated and non-deuterated aminobenzenesulfonamide molecules were designed and synthesized, and their potential application as epidermal growth factor receptor (EGFR) inhibitors for non-small cell l...
Design and synthesis of O-benzoyl amidoxime derivatives as novel TLR2/1 agonists with potent anti-radiation activity in mice [0.03%]
设计并合成新型TLR2/1激动剂O-苯甲酰基羟胺衍生物作为潜在的抗辐射候选药物
Hanyin Feng,Zhongyu Qi,Lin Pan et al.
Hanyin Feng et al.
In this paper, a series of O-benzoyl amidoxime derivatives were designed and synthesized as TLR2/1 small-molecule agonists. Among the target compounds, A-18 exhibited potent activity in human TLR2 and TLR1 transient-cotransfected HEK 293 T ...
Synthesis and evaluation of new 2-substituted anthra[2,3-b]furan-5,10-diones: tumor cell apoptosis through DNA binding and topoisomerases inhibition [0.03%]
新型2-取代蒽并芳酮的合成及抗肿瘤活性评价：通过DNA结合和抑制拓扑异构酶诱导肿瘤细胞凋亡
Alexander S Tikhomirov,Lyubov G Dezhenkova,Yulia L Volodina et al.
Alexander S Tikhomirov et al.
The clinical utility of anthracyclines is limited by severe cardiotoxicity and multidrug resistance (MDR) necessitates the development of improved analogues and new chemotherapeutics. In this work a series of 2-substituted 4,11-diaminoanthr...
A multifunctional hydrogel for synergistic dendritic cell activation and immunogenic cell death induction in enhanced chemoimmunotherapy [0.03%]
一种多功能水凝胶在增强化疗免疫治疗中的协同作用：激活树突状细胞和诱导免疫原性细胞死亡
Xiaohang An,Wenwen Yan,Yaqi Wang et al.
Xiaohang An et al.
Current cancer immunotherapies are often limited by suboptimal efficacy and significant adverse effects. Strategies centered on immunogenic cell death (ICD) offer promising solution, yet monotherapies frequently fail to achieve complete tum...
Design, synthesis and biological evaluation of novel quinolinone derivatives as potential hypoglycemic agents with hepatorenal protective effects [0.03%]
一类具有降糖及肝肾保护作用的新型喹啉酮衍生物的设计、合成与活性研究
Ruifeng Wang,Shuihua Liu,Ke Chen et al.
Ruifeng Wang et al.
Promoting glucose utilization is a pivotal strategy for reducing blood glucose, which primarily involves directly enhancing tissue uptake and consumption to effectively clear circulating glucose. Based on the promising lead compound S6 deve...
Novel anticancer alkyl pyridinium derivative exhibits antiproliferative activity via G0/G1 cell cycle arrest and apoptosis activation in triple-negative breast cancer cells [0.03%]
新颖的抗癌烷基吡啶𬭩衍生物通过G0/G1细胞周期停滞和促凋亡作用发挥抗增殖活性以抑制三阴性乳腺癌细胞生长
Nasim Rasafar,Laura A Sanchez-Michael,Angel Torres et al.
Nasim Rasafar et al.
Triple-negative breast cancer (TNBC) remains one of the most aggressive and treatment-resistant subtypes of breast cancer, urgently demanding novel therapeutic strategies. In this study, we report the synthesis, structure, physicochemical c...
Hydrocarbon stapling strategy and antitumor activity of antimicrobial peptide Lasioglossum III [0.03%]
取链细菌素Lasioglossum III的烃基连接策略及抗肿瘤活性研究
Jinqiu Li,Jiayi Zhu,Xinhao Wei et al.
Jinqiu Li et al.
The identification of novel candidate molecules with breakthrough potential is critical for advancing breast cancer therapy. Lasioglossum-III (LL-III), a linear peptide isolated from wild bee venom, has emerged as a promising lead compound ...
Exploring the potential of heterocyclic-containing tail approach in the development of novel covalent inhibitors dual-targeting EGFR and HER-2: design, synthesis and biological evaluation [0.03%]
含杂环尾部结构的共价抑制剂双靶向EGFR和HER-2的研究：设计、合成及生物活性评价
Shuang Hao,Jing-Han Yan,Rui Wang et al.
Shuang Hao et al.
Based on the structure of the existing drug afatinib, this study employed the heterocyclic-containing tail modification strategy to design and synthesize a series of novel pyrimidine derivatives, aiming to develop highly selective and low-t...
Intracellular oxygen monitoring and oxygen demand assessment using Ir(ppy)3-encapsulated polymeric micelles [0.03%]
利用封装Ir(ppy)3的高分子聚合物胶束进行细胞内氧监测及耗氧量评估研究
Narufumi Kitamura,Keiji Kajiwara,Shoichi Yamamoto et al.
Narufumi Kitamura et al.
Intracellular oxygen concentration is a pivotal indicator of cellular metabolic and functional states that may be influenced by pathologic conditions, including hypoxia in solid tumors and hyperglycemia. Currently, methods for quantifying c...
Incorporation of an alpha-hydroxy substituent modulates activity of triazole bisphosphonate-based geranylgeranyl diphosphate synthase inhibitors [0.03%]
α-羟基取代基的引入可调节三唑双膦酸类牻牛儿牻牛儿基焦磷酸合酶抑制剂的作用机制
Md Ayub Ali,Dan Feng,Staci L Haney et al.
Md Ayub Ali et al.
Geranylgeranyl diphosphate synthase (GGDPS), the enzyme responsible for producing the isoprenoid substrate used in protein geranylgeranylation reactions, represents a novel therapeutic target in cancer, including malignancies such as multip...