Design, synthesis and biological evaluation of novel 3,4-dihydro-2(1 H)-quinoline- O-carbamate derivatives as AChE/MAO-B dual inhibitors for the treatment of Alzheimer's disease [0.03%]
设计、合成及生物活性评估新型3,4-二氢-2(1H)-喹啉-O-碳酰胺衍生物作为AChE/MAO-B双通道抑制剂以治疗阿尔茨海默病
Wenling Fu,Keren Wang,Hongsong Chen et al.
Wenling Fu et al.
Alzheimer's disease (AD) is an irreversible degenerative disorder of the brain, and there is no effective drug for it to date. Given its complex pathogenesis, the multi-target-directed ligand (MTDL) strategy is considered as a promising app...
Yao Zhang,Fule Wu,Muneeb Ur Rehman et al.
Yao Zhang et al.
Natural resources have served as a cornerstone for the discovery of innovative pharmaceutical compounds for millennia. Among the diverse natural compounds demonstrating significant pharmacological activities, carbolines cannot be overlooked...
Discovery of GBA-16-24 as a highly potent, selective ATR inhibitor for the treatment of FLT3-mutated acute myeloid leukemia [0.03%]
高选择性、强效的ATR抑制剂GBA-16-24可治疗FLT3突变急性髓系白血病
Ping Li,Haiyan Ren,Xinyan Lan et al.
Ping Li et al.
Ataxia telangiectasia mutated and RAD3-related (ATR) kinase supports cancer cell survival via managing DNA damage or replication stress in various cancers, including acute myeloid leukemia (AML). Pharmacological inhibition of ATR has emerge...
Discovery of dihydrospiro[cyclopropane-1,7'-pyrrolo[3,4- d]pyrimidine] derivatives as novel ATR inhibitors [0.03%]
新型ATR抑制剂二氢螺环[环丙烷-1,7’-吡咯并[3,4-d]嘧啶]衍生物的发现
Xiaozhen Chen,Yunbo Qian,Yitong Guo et al.
Xiaozhen Chen et al.
Ataxia telangiectasia and Rad3-related (ATR) kinase plays a critical role in the DNA damage response (DDR), making it a promising target for cancer therapy. Herein, a series of dihydrospiro[cyclopropane-1,7'-pyrrolo[3,4-d]pyrimidine] deriva...
Xue Li,Yuechen Qian,Jiongjia Cheng et al.
Xue Li et al.
Peptide-drug conjugates (PDCs) represent an emerging class of targeted therapeutics engineered to enhance drug specificity and minimize systemic toxicity, showing significant promise for treating complex diseases. The peptide component is c...
Design, synthesis and biological assessment of erlotinib-1,2,3-triazole derivatives for anticancer applications [0.03%]
设计、合成和生物评估厄洛替尼-1,2,3-三氮唑衍生物用于抗癌应用
Qiyan Yao,Kexin Qu,Lan Wang et al.
Qiyan Yao et al.
Current therapeutic strategies for hepatocellular carcinoma (HCC) primarily rely on multi-targeted small molecule agents and immune checkpoint inhibitors. However, clinical trials have demonstrated limited efficacy of erlotinib monotherapy ...
Bisarylthiourea comprising cycloalkyl-thiophene-3-carboxylate derivatives as potential human toll-like receptor (TLR2) agonists: design, synthesis, and structure-activity relationship enabling the switch from TLR2/1 to TLR2/6 activation [0.03%]
环状烷基噻吩-3-羧酸衍生物双芳基硫脲类人类 Toll 样受体(TLR2)激动剂：设计、合成及结构活性关系，可实现从TLR2/1到TLR2/6激活的转换
Munugala Chandrakanth,Yoshikazu Honda-Okubo,Arya C G et al.
Munugala Chandrakanth et al.
Toll-like receptor 2 (TLR2) acts as a pivotal family of pattern-recognition receptors that bridges innate and adaptive immunity through the detection of PAMPs and DAMPs. In pursuit of novel immunomodulators, a series of bisarylthiourea (BAT...
Pankaj Gupta,Sangeeta Verma,Rakesh Narang et al.
Pankaj Gupta et al.
Antimicrobial resistance (AMR) has emerged as a major worldwide issue in the effective management of infectious diseases. This problem prompted researchers worldwide to develop new therapeutic agents that target both well-established and no...
PROTAC-mediated multi-target protein degradation in Alzheimer's disease: mechanistic insights, therapeutic applications, and translational challenges [0.03%]
阿尔茨海默病的PROTAC介导的多蛋白降解：机制、治疗和转化挑战
Bin Wang,Yunan Li,Tingting Yao et al.
Bin Wang et al.
Alzheimer's disease (AD) is a progressive neurodegenerative disorder characterized by multiple interacting pathological mechanisms. Among these, the core driving factor is the accumulation of abnormally folded, neurotoxic proteins. Current ...
ZRMQ-22, a novel DYRK1A inhibitor, attenuates neuroinflammation and cognitive impairments in LPS-induced mice: a potential strategy for Alzheimer's disease [0.03%]
新型DYRK1A抑制剂ZRMQ-22通过减轻脂多糖诱导的小鼠神经炎症和认知障碍抑制阿尔茨海默病的潜在策略研究
Mengyu Ren,Huanhua Chen,Zhenshu Li et al.
Mengyu Ren et al.
Alzheimer's disease (AD) is a progressive neurodegenerative disorder characterized by irreversible cognitive decline and memory loss. Targeting the kinase DYRK1A has emerged as a promising therapeutic strategy, as it plays a critical role i...