Benzoxaboroles Are Inhibitors of the η-Class Carbonic Anhydrase From Plasmodium falciparum [0.03%]
苯并恶硼类化合物是恶性疟原虫η类碳酸酐酶的抑制剂
Alessandro Bonardi,Sharon Wein,Muhamad Mustafa et al.
Alessandro Bonardi et al.
Malaria remains a major global health burden, compounded by increasing resistance to current therapies. Plasmodium falciparum carbonic anhydrase (PfaCA), a η-class metalloenzyme essential for the parasite metabolism and survival, has recen...
Acetylcholinesterase and Carbonic Anhydrase Inhibition Profiles of New 5-HMF Chalcones and Their Ester Derivatives [0.03%]
新的5-HMF查尔康和相应的酯类衍生物的乙酰胆碱酯酶和碳酸酐酶抑制研究
Ayşe İlhan,Ferhat Güneş,Adem Ertürk et al.
Ayşe İlhan et al.
Acetylcholinesterase (AChE) is one of the most important therapeutic targets in the treatment of neurological disorders such as Alzheimer's disease. In recent years, studies on the use of carbonic anhydrase (CA) inhibitors in the treatment ...
Sustainable Synthesis and Medicinal Profiling of Azo-Anchored Imidazo[4,5-b]Indole Scaffolds: DFT Studies, Electrochemical Sensing, and Pharmacokinetic Evaluation [0.03%]
偶氮连接的imidazo[4,5-b]吲哚支架的可持续合成和药物轮廓分析：DFT研究，电化学传感和药代动力学评估
Deepika Geedkar,Ashok Kumar,Rashmi Sharma et al.
Deepika Geedkar et al.
The synthesis of azo-anchored imidazo[4,5-b]indoles represents a promising advancement in therapeutic and sensor technologies, offering significant potential in biomedical applications. This study presents a sustainable, high-yield approach...
HBE-843, a Novel, Potent, and Selective EGFR Targeting PROTAC for the Treatment of Non-Small-Cell Lung Cancer [0.03%]
新型、有效且特异的靶向EGFR肺癌治疗PROTAC药物HBE-843
Mohammad Hassan Baig,Chang Joong Kim,Nale Sagar Dattatraya et al.
Mohammad Hassan Baig et al.
The emergence of the EGFR C797S mutation poses a significant challenge in the treatment of non-small cell lung cancer due to resistance to third-generation EGFR-tyrosine kinase inhibitors. This study introduces a novel and highly selective ...
FOLR1 Mediated by ITCH Promotes Paclitaxel Resistance by Suppressing Pyroptosis in Nasopharyngeal Carcinoma [0.03%]
ITCH介导的FOLR1通过抑制焦亡促进鼻咽癌多西他赛耐药性
Gehou Zhang,Yexun Song,Honghui Liu et al.
Gehou Zhang et al.
Paclitaxel is a frequently employed chemotherapeutic agent for nasopharyngeal carcinoma (NPC) patients, and tumor cell resistance to paclitaxel poses a significant challenge to NPC treatment. This study investigated the impact and potential...
Algal-Bacterial Interaction-Driven Secondary Metabolites From Phaeobacter inhibens and Their Anti-Allergic Effects on Th2 Cell Immune Response [0.03%]
玫瑰色海洋发光菌次生代谢产物及其对Th2型免疫反应的抗过敏作用
Jisu Kim,Soo-Jin Park,Yeo Jin Lee et al.
Jisu Kim et al.
The Roseobacter clade, a versatile Rhodobacteraceae lineage, comprises up to 20% of marine bacteria and drives key biogeochemical cycles. Phaeobacter inhibens, a representative model species, is associated with the alga Emiliania huxleyi, e...
Targeting EGFR With Quinazoline-4-One/Chalcone Hybrids: Design, Synthesis, and Anticancer Evaluation [0.03%]
喹唑啉-4-酮/查尔康素杂化物靶向作用于EGFR的设计、合成及抗肿瘤活性评价
Yomna I El-Gazzar,Rasha Abdelhady,Nancy S Younis et al.
Yomna I El-Gazzar et al.
A series of novel quinazoline-4-one/chalcone hybrids (4a-4j) were synthesized and evaluated as epidermal growth factor receptor (EGFR) inhibitors with anticancer activity. The target compounds were in vitro tested against MCF-7 and HepG2 ca...
Role of Brusatol in Preventing Gastrointestinal Cancer: Recent Trends and Future Perspectives [0.03%]
溴沙坦防治胃肠癌的作用机制及展望趋势分析
Falak Thakral,Rippin Sehgal,Gagandeep Singh et al.
Falak Thakral et al.
Gastrointestinal (GI) cancers represent a major global health burden due to their high incidence and mortality. Brusatol has emerged as a promising natural anticancer agent with potent activity against diverse malignancies. It exerts antitu...
Activity Profiling of Nitro-Substituted Di(Hetero)Aryl 1,3,4- and 1,2,4-Oxadiazoles: Antimicrobial, Cholinesterase Inhibition and Antioxidant Potential [0.03%]
硝基取代的二（杂）芳基-1,3,4-和1,2,4-恶二唑活性谱研究：抗菌，胆碱酯酶抑制及抗氧化性能
Enikő Šikorová,Šárka Štěpánková,Eva Frýbová et al.
Enikő Šikorová et al.
Oxadiazole derivatives represent a promising scaffold for drug discovery, offering therapeutic potential, notably against neurodegenerative diseases and microbial infections. Based on molecular hybridisation approach utilising bioactive oxa...
Retrospection of the USFDA-Approved Halogenated Drugs and Their Implication in Medicinal Chemistry and Drug Discovery: A Perspective of Approved Drugs Between 2019 and 2024 [0.03%]
从美国食品药品监督管理局获批的含卤素药物展望药物设计与发现：2019—2024年获批药物的启示
Nemat Ali,Fahad T Alotaibi,M Arockia Babu et al.
Nemat Ali et al.
Halogens are utilized in drug discovery and development due to their ability to precisely tune the molecular properties of drug candidates. The halogen substituents play a crucial role in determining the stability, lipophilicity, and recept...