Wee1-targeting inhibitors: From virtual screening to lead discovery [0.03%]
从计算机虚拟筛选到先导化合物发现——Wee1靶向抑制剂研究
Jochem Nelen,Bidisha Sarkar,Javier Jiménez-Bernad et al.
Jochem Nelen et al.
Wee1-like protein kinase (Wee1) is a validated target for cancer therapy, though no inhibitors have yet received regulatory approval. To identify new Wee1 inhibitors, we conducted a virtual screening campaign using the Eurofins-Villapharma ...
Design, synthesis and biological evaluation of benzimidazole carbamide derivatives - potential autophagy inducers [0.03%]
苯并咪唑碳酰胺衍生物的设计、合成及生物活性评价——潜在的自噬诱导剂
Maria V Zapevalova,Ekaterina A Guseva,Sofya Y Sokolskaya et al.
Maria V Zapevalova et al.
Herein, we report a convenient synthetic approach and an in vitro evaluation of benzimidazole carbamide derivatives as potential autophagy activators. Two compounds exhibited autophagy-inducing activity at concentrations ≥100 μM. The most...
Synthesis and pharmacological evaluation of benzimidazole amine derivatives as novel allosteric antagonists for β2-adrenergic receptor [0.03%]
一类新型β2-肾上腺素受体变构拮抗剂的苯并咪唑胺类衍生物的设计、合成及药理评价研究
Yu Chen,Kexin Ye,Yujie Zhang et al.
Yu Chen et al.
Based on the previous research addressing the insufficient stability of benzimidazole amide derivatives, in this study we synthesized two novel classes of the allosteric antagonists for the β2-adrenergic receptor (β2AR) through structural...
Development of highly potent EP2 antagonists as novel anti-inflammatory neuroprotectants [0.03%]
高效EP2拮抗剂的开发作为新型抗炎神经保护剂
Chenyao Jiang,Eun Bee Cho,Zhen Jin et al.
Chenyao Jiang et al.
Prostaglandin E2 (PGE2) is a key bioactive lipid mediator that drives neuroinflammation and exacerbates brain tissue damage largely via acting on its receptor EP2 subtype. As such, EP2 has been emerging as an alternative target to cyclooxyg...
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...