A Rofecoxib-Derived Theranostic Probe and Its Combination With PD-1 Inhibitor for High-Efficiency Cancer Therapy [0.03%]
一种罗非考昔派生的诊疗探针及其与PD-1抑制剂联合用于高效癌症治疗
Xinli Wang,Xia Wang,Xuejing Su et al.
Xinli Wang et al.
The development of theranostic probes with tumor-specific targeting and high therapeutic efficacy remains a pivotal challenge in precision oncology. Herein, we have successfully developed a new cyclooxygenase-2 (COX-2)-targeted probe compou...
Recent Advancements and Developments of Anti-Malarial Agents Reported in 2023 [0.03%]
2023年抗疟药物研究进展与发展近况
Palak K Vadodariya,Shahnaz Alom,Anu Sharma et al.
Palak K Vadodariya et al.
Malaria, caused by Plasmodium falciparum and other species, remains a significant global health issue, transmitted by infected Anopheles mosquitoes. According to the WHO 2024 report, malaria affected 249 million individuals and resulted in ...
Solvent and Catalyst-Free One-Pot Synthesis of Tetrahydropyrimidine Analogs for Their Larvicidal Activity and Structural Insights [0.03%]
无需溶剂和催化剂的一锅法合成四氢嘧啶类似物及其幼虫杀灭活性和结构洞察
Keshab M Bairagi,Sandeep Chandrashekharappa,Jyoti Swarup Thakur et al.
Keshab M Bairagi et al.
A series of ester derivatives of (6-methyl-4-phenyl-2-thioxo-1, 2, 3, 4-tetrahydropyrimidin-5-yl)(piperidin-1-yl) methanone (6a-6k) have been synthesized using a solvent and catalyst-free one-pot two-step synthetic method. These 11 molecule...
New Se-Compounds With Antileishmanial, Antitumor, and Carbonic Anhydrase Inhibitory Properties [0.03%]
具有抗利什曼病、抗肿瘤和碳酸酐酶抑制性能的新化合物
Cristina Morán-Serradilla,Daniel Plano,Andrea Angelli et al.
Cristina Morán-Serradilla et al.
In the pursuit of novel agents for treating leishmaniasis and cancer, we have synthesized a small library of phenylcarboxamide-selenium analogs and evaluated their in vitro antileishmanial, anticancer, and carbonic anhydrase inhibitory acti...
Phenylvinylsulfonate-Anchored Azetidin-2-ones as Potent Antibacterial Agents: ROS-Mediated Mechanism, Selective Cytotoxicity, and In Silico Target-Interaction Studies [0.03%]
苯乙烯基磺酸盐连接的氮杂缩酮作为有效的抗菌剂：ROS介导的作用机制，选择性细胞毒性和计算机辅助药物作用靶点研究
Shalu Thakur,Rohit Sharma,Nishima Wangoo et al.
Shalu Thakur et al.
The rise of multidrug-resistant pathogens, including MRSA, underscores the urgent need for novel antibacterial agents with minimum resistance potential and enhanced potency. Herein, we report the design and synthesis of novel phenylvinylsul...
Design, Synthesis, and Selective Antiproliferative Activity of Indolizine Derivatives as Microtubule Destabilizers [0.03%]
作为微管解稳剂的吲哚嗪衍生物的设计、合成及选择性抗增殖活性研究
Victor Hugo Catricala Fernandes,Maitê Bueno Giometti,Franco Jazon Caires et al.
Victor Hugo Catricala Fernandes et al.
The development of selective anticancer agents with minimal off-target toxicity remains a major therapeutic goal. In this study, we synthesized and evaluated a series of 32 indolizine derivatives for antiproliferative activity against oral ...
Recent Advances in the Biological Activities of Monocarbonyl Curcumin Analogues (MACs) [0.03%]
单羰基类姜黄素类似物(MACs)的最新生物活性研究进展
Amol A Nagargoje,Sharad P Panchgalle,Madiha M Siddiqui et al.
Amol A Nagargoje et al.
Curcumin, a principal component of the Indian spice turmeric, exhibits a wide range of biological activities but suffers from poor pharmacokinetic and pharmacodynamic profiles. To overcome these limitations, monocarbonyl analogues of curcum...
Reevaluating 1,3-Thiazolidinone Reports: Deciphering the Authentic 1,3-Thiazolidinone Frameworks via Synthetic and Spectroscopic Insights [0.03%]
重新评估1,3-噻唑啶酮报道：通过合成和光谱学洞察解析真实的1,3-噻唑啶酮框架
Roghayeh Hosseininia,Farough Nasiri
Roghayeh Hosseininia
Accurate structural determination of heterocyclic scaffolds is essential for medicinal chemistry and drug discovery. In this study, products obtained from three-component reactions of aryl isothiocyanates, dialkyl acetylenedicarboxylates, a...
C-5-Arylidene-Thiazolidine-2,4-Dione Analogs Against Aldose Reductase: Design, Synthesis, Biological Evaluation, and Computational Insights [0.03%]
设计、合成及生物活性评价一系列新型噻唑烷二酮类似物作为醛糖还原酶抑制剂及其分子机制研究
Rajiv Patel,Sanjeev Ranjan,Nandini et al.
Rajiv Patel et al.
Diabetic complications are major health problems that happen to people with diabetes when their blood sugar levels stay high for a long time and damage various body organs and systems. Inhibition of aldose reductase has emerged as a promisi...
Mechanistic Insights into the Anticancer Potential of Echinacoside: Therapeutic Applications and Future Directions [0.03%]
番红花苷抗肿瘤潜力的机制见解：治疗应用和未来方向
Anju Sheokand,Dolly Koli,Karan Wadhwa et al.
Anju Sheokand et al.
Echinacoside, a naturally occurring phenylethanoid glycoside, primarily derived from medicinal plants such as Cistanche tubulosa and Echinacea angustifolia, has long been valued in traditional medicine for its diverse pharmacological activi...