Synthesis of Some Novel Chalcone and 3,5-Disubstituted Pyrazoline Derivatives: Evaluation of Their α-Amylase and α-Glucosidase Inhibitory Activities In Vitro and In Silico [0.03%]
一些新型查耳酮和3,5-取代吡唑啉衍生物的合成及其体内外α-淀粉酶和α-糖苷酶抑制活性评价
Fatma Erbay,Melike Yildirim Akatin,Fatma Demir et al.
Fatma Erbay et al.
This study reports the synthesis of some novel chalcone (C1-C3) and 3,5-disubstituted pyrazoline derivatives (P1-P3), structurally based on aminophenyl and trifluoromethylphenyl groups. Their potential as antidiabetic agents was evaluated t...
Indicaxanthin Mitigates Hepatic Ischemia Reperfusion Injury in Rats via Bax/Bcl-2 Modulation: Experimental Evidence Supported by Molecular Docking and Dynamics Simulation [0.03%]
天冬红素通过调节Bax/Bcl-2缓解大鼠肝脏缺血再灌注损伤：实验证据结合分子对接和动力学模拟支持
Mahmoud Abdelnaser,Abeer H Elmaidomy,Mina Ezzat Attya et al.
Mahmoud Abdelnaser et al.
Indicaxanthin, a prominent betalain pigment known for its bioactivity and safety, has long been valued in traditional medicine for its antioxidant and anti-inflammatory effects. The leading cause of liver failure and dysfunction is hepatic ...
New Sinomenine Derivative as a Potential Drug for Cervical Cancer via Inducing Ferroptosis [0.03%]
一种新的青风藤素衍生物通过诱导铁死亡潜在地用于治疗宫颈癌
Yifan Shang,Keran Li,Wenting Liu et al.
Yifan Shang et al.
Cervical cancer remains a serious threat to women's health due to chemotherapy resistance, poor prognosis, and survival rates. Novel anti-cervical cancer agents are urgently needed. Sinomenine derivatives, which were prepared from sinomenin...
Bodipy-Labeled Allopregnanolone: Synthesis, GABAA Receptor Positive Allosteric Modulation, In Silico Binding Pose Determination and Neurons Staining [0.03%]
Bodipy标记的别孕烷二醇：合成，GABAA受体阳性变构调节，计算机上确定结合姿势和神经元着色
Sergey N Kolbaev,Denis Y Uvarov,Natalia Smirnova et al.
Sergey N Kolbaev et al.
The first BODIPY-allopregnanolone conjugates have been synthesized by selecting the C21 position for labeling. The steroidal moiety and BODIPY fluorophores were coupled through flexible amino acid-derived linkers, designed with rotatable bo...
New Benzimidazole Scaffolds Tagged With Isatin/Thiourea Motifs as Anti-Cancer Agents: Promising Approach for VEGFR-2 Inhibition [0.03%]
具有异噻唑/硫脲基元的新型苯并咪唑抗肿瘤剂作为抑制VEGFR-2的有前景的方法
Alaa M Ali,Bhoomendra A Bhongade,Samar S Tawfik et al.
Alaa M Ali et al.
Inspired by the structural insights of the reported kinase inhibitor Sorafenib, two new series comprising 19 benzimidazole-based compounds incorporating isatin and thiourea motifs were rationally designed as a novel VEGFR-2-targeting anti-c...
Therapeutic Horizons in Targeting EZH2 With Dual and Non-PROTAC Inhibitor Molecules: Recent Achievements, Comparative Analysis, and Future Perspectives [0.03%]
靶向EZH2的双效和非PROTAC抑制剂分子的治疗前景：近期成就、比较分析及未来展望
Hamada S Abulkhair
Hamada S Abulkhair
The aberrant overexpression of Enhancer of Zeste Homolog 2 (EZH2) endorses uncontrolled cell proliferation and metastasis across multiple malignancies. These make EZH2 an attractive biological target for the development of potential antican...
Sideroxylonal B: A Dimeric Phloroglucinol From Eucalyptus cinerea With In Vitro Carbonic Anhydrase Inhibition and Evaluation of Cytotoxicity and Antiviral Potential [0.03%]
侧链木脂素B：一种来自Eucalyptus cinerea的二聚菲 glucinol，具有抑制碳酸酐酶的活性及细胞毒性和抗病毒潜力的评估
Fatema R Saber,Alessandro Bonardi,Rasha A Hassan et al.
Fatema R Saber et al.
Sideroxylonal B, a natural dimeric acylphloroglucinol, demonstrates promising anticancer potential through a dual mechanism of action involving both cytotoxicity and selective enzyme inhibition. In preliminary screening against the NCI 60 h...
Imidazo[1,2-a]Pyridine Derivatives as Promising Anticancer Agents: Synthesis and Therapeutic Potential [0.03%]
咪唑并吡啶衍生物作为有前景的抗肿瘤剂：合成与治疗潜力研究
Drashti Shah,Ashish Patel
Drashti Shah
Heterocyclic compounds play a crucial role in medicinal chemistry, with imidazo[1,2-a]pyridine emerging as a significant scaffold due to its broad pharmacological applications. The unique structural framework of imidazo[1,2-a]pyridine allow...
Design, Synthesis and Evaluation of Indole-Based 1,2,3-Triazoles as Potential Quorum Sensing and Biofilm Inhibitors Against Pseudomonas aeruginosa [0.03%]
基于吲哚的1,2,3-三唑的设计、合成及评价其作为潜在群体感应和生物被膜抑制剂对抗绿脓杆菌的作用
Kosana Sai Chaitanya,Tsz Tin Yu,Hrushikesh Chaudhari et al.
Kosana Sai Chaitanya et al.
Targeting quorum-sensing inhibitors (QSIs) is a promising strategy to combat antibiotic-resistant bacteria by disrupting biofilm formation without imposing direct lethal pressure. In this study, we designed and synthesized a library of 30 2...
Investigating the Telomerase Downregulatory Potential of Steroidal Drugs Following Pharmacophore-Based Rational; Computational and In Vitro Assessments [0.03%]
基于药效团的合理计算及体外评估下的类固醇药物下调端粒酶潜能的研究
Ahmed A Al-Karmalawy,Aya Yaseen Mahmood Alabdali,Tarek A Yousef et al.
Ahmed A Al-Karmalawy et al.
Inhibiting telomerase could lead to telomere shortening, chromosomal instability, and eventually cell death in cancer cells. The use of steroids in cancer treatment is significant; besides, drug repurposing can be a quicker and less expensi...