Screening of Novel Inhibitors Targeting the Non-ATP-binding Domain of Staphylococcus aureus SecA1 [0.03%]
靶向金黄色葡萄球菌SecA1非ATP结合区的新型抑制剂筛选
Yan Liu,Qing Su,Zonglin Wang et al.
Yan Liu et al.
Objective: Staphylococcus aureus (S. aureus) has been one of the pathogenic bacteria for clinical infections, and there is an urgent need for the development of novel anti-S. aureus drugs. SecA is a conserved and essentia...
Design and Synthesis of (2,3-dichloro-4-(3-(substituted Phenyl)acryloyl) phenoxy) Substituted Carboxylic Acid as Potent Glutathione-s-transferase Inhibitors, Anti-breast-cancer Agents and Enhancing Therapeutic Efficacy of Anticancer Agents [0.03%]
设计并合成（2，3-二氯-4-（3-（取代苯基）丙烯酰基）苯氧代）羧酸衍生物作为谷胱甘肽-s-转移酶抑制剂、抗乳腺癌制剂及抗癌药物增效剂
Afreen Begum Abdul Qayyum,Syed Ayaz Ali,Santosh Namdeo Mokale
Afreen Begum Abdul Qayyum
Background: Ethacrynic acid is a dynamic agent holding alpha-beta unsaturated carbonyl unit in its structure which imparts superiority and extraordinary advantage of displaying multiple biological activities such as antic...
Synthesis, Characterization, and In Vitro and In Silico Studies of New Triazole Derivatives as Aromatase Inhibitors [0.03%]
三唑衍生物类芳香化酶抑制剂的合成、表征及体内外研究
Zeynep Livanur Uzmez,Derya Osmaniye,Yusuf Ozkay et al.
Zeynep Livanur Uzmez et al.
Introduction: Breast cancer is the most common type of cancer among women. Steroidal or non-steroidal aromatase inhibitors (NSAIs) are used clinically, and in most cancer diseases, resistance is the most important problem...
In Silico Analysis and Molecular Docking of Human Antimicrobial Peptides for Targeting Monkeypox Virus: Potential Therapeutic Implications of Histatin 5 Peptide [0.03%]
组蛋白衍生物His5的抗猴痘病毒活性及作用机制研究
Deeksha Sarojini Devi Radhakumar,Sundar Thiyagarajan,Kaushik Rajaram et al.
Deeksha Sarojini Devi Radhakumar et al.
Background: Monkeypox, a viral zoonotic disease akin to smallpox, has posed significant public health challenges, particularly in Africa. Recent outbreaks, including those in India, underscore the global threat it poses. ...
Pharmacological Evaluation of Bioisosterically Replaced and Triazole- Tethered Derivatives for Anticancer Therapy [0.03%]
用于抗癌治疗的生物等排体取代和三唑连接衍生物的药理学评价
Dipesh Kumar,Salahuddin,Avijit Mazumder et al.
Dipesh Kumar et al.
Cancer has been the cause of the highest number of deaths in the human population despite the development and advancement in treatment therapies. The toxicity, drug resistance, and side effects of the current medicaments and therapies have ...
One-Pot Synthesis of Benzoxazoles: A Promising Approach to Aromatic Heterocyclic Compounds Preparation [0.03%]
一步合成苯并噁唑：一种制备芳香杂环化合物的有前景的方法
Monika Chauhan,Sumitra Nain
Monika Chauhan
Considering the necessity for broad synthetic operations, integrating various reactions into a single pot operation is an intriguing approach to improve synthetic efficiency. One-pot operations may serve as an effective way to minimize the ...
Inhibitors of Phosphatidylinositol-specific Phospholipase C with Myo-inositol Scaffold [0.03%]
具有肌醇支架的磷脂酰肌醇特异性磷脂酶C抑制剂
Christian Bierkamp,Walburga Hanekamp,Christoph Arenz et al.
Christian Bierkamp et al.
Background: Phosphatidylinositol-specific phospholipase C (PI-PLC) enzymes catalyze the conversion of phosphatidylinositol-4,5-bisphosphate into the second messengers diacylglycerol and inositol- 1,4,5-trisphosphate, both...
Design, Synthesis, and Biological Evaluation of a Novel Series of Thiazolidinediones as Dual GSK-3ß and Tau Aggregation Inhibitors [0.03%]
一类新型噻唑烷二酮衍生物的设计、合成及生物学评价：兼有GSK-3β抑制和Tau蛋白聚集抑制活性
Zahra Abdollahi,Khalil Abnous,Mohamad Reza Kalani et al.
Zahra Abdollahi et al.
Introduction: Glycogen synthase kinase-3β (GSK-3β) is a serine/threonine kinase that is involved in the synthesis of glycogen. Among the inhibitors, thiazolidinediones (TZDs) can specifically bind to GSK-3ß. They act n...
Curcumin-Based Virtual Screening Identifies Inhibitors of SARS-CoV-2 Spike Protein and ACE2 Receptor Binding [0.03%]
基于姜黄素的虚拟筛选识别SARS-CoV-2刺突蛋白和ACE2受体结合抑制剂
Timoteo Delgado-Maldonado,Luis D Gonzalez-Morales,Gilberto Vargas-Salas et al.
Timoteo Delgado-Maldonado et al.
Background: To date, COVID-19 has caused over 772 million cases, with approximately 7 million deaths, according to the World Health Organization. Therefore, there is a need to develop new drugs to address the challenges p...
Scaffold Hopping and Optimization of Thiazole Hybrids as Selective PIN1 Inhibitors: A Computational Study [0.03%]
计算研究噻唑杂化物作为选择性PIN1抑制剂的药物支架跃迁和优化
Meeramol C Chellappan,Soumya Vasu,Shriraam Mahadevan et al.
Meeramol C Chellappan et al.
Background: Protein Interacting with NIMA1 (PIN1) is a distinct enzyme, known as a peptidyl-prolyl cis-trans isomerase (PPIase), which catalyzes the cis-trans isomerization of amide bonds in proteins containing phosphoser...