Targeting Human Protein Kinase CK2 by a Library of Indeno[1,2-b]Indoles: Contribution of Thermal Shift Assay to Pre-Screening and Co-Crystallization to Post-Screening [0.03%]
靶向人蛋白激酶CK2的吲哚并苯并_indeno[1,2-b]indole类库：热移法在预筛选和共结晶在后筛选中的贡献
Matheus M Guimarães,Christian Werner,Belen Leroy et al.
Matheus M Guimarães et al.
Protein kinase CK2 is the subject of numerous studies in medicinal chemistry due to its involvement in the development of several diseases, primarily cancers. Its overexpression in tumor cells is related to key processes such as tumor immun...
4-(5'-Dimethylamino)-Naphthalenesulfonyl-2(3H)-Benzoxazolone (W3D) Ameliorated COPD Lung Injury Through Regulating Macrophage Polarization Mediated by Glycolysis [0.03%]
4'-（二甲氨基）-1-萘磺酰基-2(3H)-苯并恶唑酮通过调节糖酵解介导的巨噬细胞极化来缓解慢性阻塞性肺疾病损伤
Qikai Su,Yichen Yang,Zhichao Ren et al.
Qikai Su et al.
Chronic obstructive pulmonary disease (COPD) remains a significant global health challenge, which urges the discovery of novel drugs. In this article, we investigated the therapeutic potential and action mechanism of a new benzoxazolone der...
Thiazole-Derived Dual EGFR/CDK-2 Inhibitors: Rational Design, Synthesis, In Vitro Anticancer Evaluation, Mechanistic Profiling, and Computational Binding Analysis [0.03%]
基于噻唑的EGFR/CDK-2双靶点抑制剂：合理设计、合成、体外抗肿瘤评价、机制分析及计算结合模式研究
Rowida Nasr,Mohamed S Nafie,Hesham Haffez et al.
Rowida Nasr et al.
New series of thiazole analogues were designed, synthesized, and tested for their potential anticancer activity. All the synthesized compounds were biologically tested against HCT-116 and MCF-7 cell lines. Compounds 14d, 14h, and 14i were d...
Evaluation of Novel Cloxyquin Analogs for K2P18.1 Channel Modulation [0.03%]
评估新型氯奎酮类似物调节K2P18.1通道的作用
Jasmin Sörgel,Marcel Kloth,Henning Klaasen et al.
Jasmin Sörgel et al.
K2P18.1 (TRESK) displays one of the most unusual two pore domain potassium channels, that is associated with different neurological and immune-related diseases emphasizing the therapeutic potential of K2P18.1 activators. Previous studies id...
Recent Overview on the Molecular Hybrids Integrated With Benzosuberone/Benzo[7]annulene Derivatives as Multi-Target Therapeutics [0.03%]
苯并角状烃/苯并七环素衍生物分子杂化物作为多靶标药物的研究进展综述
Mohamed S Nafie,Kamal M Dawood,Mohamed K Diab et al.
Mohamed S Nafie et al.
Benzosuberone is a promising scaffold with a remarkably varied pharmacological profile that has been attracting significant interest in the potential development of anticancer agents. This review focuses on the historical interest, diversit...
Total Synthesis of Marine Natural Product Sunshinamide via Macrolactonization [0.03%]
海洋天然产物Sunshinamide的全合成——巨环化策略
Yi Lu,Yuanmu Zhang,Hanqi Wang et al.
Yi Lu et al.
A new approach for the synthesis of marine natural product Sunshinamide has been developed, featuring macrolactonization as a key step. The important synthetic strategy is to first construct the unique 8-membered cyclic dithiazocane in the ...
Mutation-Induced Pocket Deactivation: How Ser353/Pro245 Alters KCa2.2 vs. KCa3.1 Ligand Selectivity [0.03%]
突变诱导的结合袋失活：Ser353/Pro245如何改变KCa2.2与KCa3.1配体的选择性
Matteo Gozzi,Joana Massa,Oliver Koch
Matteo Gozzi
The KCa2.2 and KCa3.1 channels are fundamental regulators of membrane potential and calcium signalling and promising targets to treat diseases such as spinocerebellar ataxia and cancer. To fully exploit their therapeutic potential, and to c...
Emerging Indole and Azaindole Hybrid Agents for Leukemia Therapy: Recent Research Advances and Therapeutic Potential [0.03%]
用于白血病治疗的吲哚和氮杂吲哚混合剂：近期研究进展与治疗潜力
Yanjing Cheng,Lianlian Chen,Danchen Zhao et al.
Yanjing Cheng et al.
Leukemia represents a heterogeneous and refractory hematological malignancy, with current clinical therapies, including conventional chemotherapy, targeted therapy, and hematopoietic stem cell transplantation, still limited by drug resistan...
Gastroprotective Activity of Myrtenol Derivatives Obtained by Biocatalytic Esterification and Photooxidation [0.03%]
由生物催化酯化和光氧化获得的甲基松油醇衍生物的胃保护作用
Ana Flávia Seraine Custódio Viana,Mateusz Kutyła,Hélio de Barros Fernandes et al.
Ana Flávia Seraine Custódio Viana et al.
Many naturally occurring substances exhibit anti-ulcer properties. One promising area of research is the identification of terpenoid compounds with enhanced therapeutic and gastroprotective properties. The present study aimed to synthesize ...
Electro-Mechanical Uncoupling of KV7.1 Voltage Sensor and Pore by 1,4-Benzodiazepines Is Modulated by Decoration of Position 1 [0.03%]
苯并二氮杂卓通过修饰位点1调节对KV7.1电压门控离子通道机械耦合的阻断作用
Florian Roßner,Thomas Jepps,Bo Hjorth Bentzen et al.
Florian Roßner et al.
The voltage-gated potassium channel KV7.1 (KCNQ1) is essential for cardiac repolarization. Loss-of-function mutations prolong the action potential and cause long QT syndrome 1, predisposing to malignant arrhythmias. Pharmacological activato...