Oxazole-4,5-dicarboxylate derivatives as multifunctional targets against oral cancer and Streptococcus mutans oral pathogens [0.03%]
氧唑-4,5-二羧酸衍生物作为多功能靶标以对抗口腔癌和变异链球菌等口腔病原体
Tamilvelan Manjunathan,Ajay Guru
Tamilvelan Manjunathan
Aims: A mild and metal free method was employed for the synthesis of various substituted oxazoles (C1-C5). These compounds demonstrated the ability to quench ROS in an in vitro antioxidant assay. The biological studies we...
Exploring thiazole conjugates as cholinesterase inhibitors for Alzheimer's disease treatment [0.03%]
用于阿尔茨海默病治疗的噻唑共轭物作为胆碱酯酶抑制剂的研究
Anchal Dabas,Parul Yadav,Ram Singh
Anchal Dabas
Alzheimer's Disease (AD), a major global health concern, is marked by memory loss and cognitive decline, especially in the elderly. Cholinergic hypothesis is one of the leading hypotheses toward the treatment of AD, prompting the developmen...
Bridging the green skills gap: a framework to align the pharmaceutical workforce with sustainable drug discovery [0.03%]
弥合绿色技能差距：一个框架，用于使制药业劳动力与可持续药物发现保持一致
Osama I Alwassil
Osama I Alwassil
Background: The pharmaceutical industry's R&D model faces unsustainable costs and environmental impact, yet educational pipelines lag in integrating AI and green chemistry skills essential for modern drug discovery. ...
LSD1-based dual-target inhibitors as emerging anticancer agents: pharmacological perspectives and SAR exploration [0.03%]
基于LSD1的双靶点抑制剂作为新兴抗肿瘤药物的药理学观点和构效关系研究
Pitam Ghosh,Ryena Dhir,Dinki Sharma et al.
Pitam Ghosh et al.
LSD1 is a key epigenetic eraser that demethylates the histone proteins and regulates transcription. Overexpression of LSD1 drives the development of multiple cancers, such as prostate, breast, gastric, lung, colorectal cancers, and acute my...
Dual HDAC/PI3K inhibitors as a potential and emerging cancer therapy: a review [0.03%]
HDAC和PI3K双靶点抑制剂作为潜在的新兴抗癌疗法：综述
Madhukumari,Akshatha Handattu Shankaranarayana,Salini P Nair et al.
Madhukumari et al.
Cancer continues to cause a major global health challenge, largely because of the heterogeneity of molecular changes that allow cancer cells to grow uncontrollably and evade therapy. The various pathways implicated include HDACs and PI3Ks, ...
Recent advances in 1,3,5-triazine-based PI3K inhibitors for cancer therapy: a comprehensive review [0.03%]
用于癌症治疗的基于1,3,5-三嗪的PI3K抑制剂最近的研究进展：全面综述
Utkarsha Kulkarni,Adarsh Yadav,Princy Desai et al.
Utkarsha Kulkarni et al.
Dysregulation of the phosphatidylinositol-3-kinase (PI3K) - AKT/mTOR signaling axis is a major molecular driver of tumor initiation, progression, and therapeutic resistance across diverse cancers, underscoring the need for improved targeted...
Indole-based carbohydrazides as potent anti-proliferative leads and tubulin polymerization inhibitors: design, synthesis, cytotoxic evaluation, in silico ADMET and docking studies [0.03%]
基于吲哚的碳胲化合物作为有效的抗增殖先导物和微管聚合抑制剂：设计、合成、细胞毒性评价、ADMET及对接研究
Aisha A Alsfouk,Eman S Nossier,Mohamed Omar et al.
Aisha A Alsfouk et al.
Aims: A novel series of indolecarbohydrazide derivatives (3a-r) was designed and synthesized to evaluate their potential as tubulin polymerization inhibitors and selective anticancer agents. ...
Dipti B Upadhyay,Mehul P Parmar,Hitendra M Patel
Dipti B Upadhyay
The serine/threonine kinase 33 (STK33) has attracted attention in recent years as a synthetic-lethal partner of oncogenic KRAS, thereby representing a potential indirect route to target KRAS-driven cancers. Initially, RNAi screens suggested...
Biological evaluation and molecular docking of previously reported pyrazolo-thiazole derivatives as dual α-amylase and α-glucosidase inhibitors [0.03%]
先前报道的吡唑并噻唑衍生物作为淀粉酶和葡萄糖苷酶双抑制剂的生物学评价及分子对接研究
Mohammed El Behery,Hagar Ahmed Elsayed,Ali H Abu Almaaty et al.
Mohammed El Behery et al.
Aim: Postprandial hyperglycemia is an important therapeutic target in type 2 diabetes mellitus. This study aimed to evaluate previously reported pyrazolo[3,4-d]thiazole derivatives as dual inhibitors of α-amylase and α-...
Coumarin derivatives as antidiabetic agents: a comprehensive review on mechanistic insights, structure-activity relationships, in silico studies, and challenges [0.03%]
香豆素衍生物作为抗糖尿病药物：对机制见解、构效关系、计算机研究以及挑战的全面综述
Salesh Verma,Sant Kumar Verma
Salesh Verma
In recent years, coumarin has been structurally modified by combining it with heterocyclic or other active pharmacophores such as thiazolidinedione, hydrazone, triazole, cinnamic acid, aza group, oxadiazole, sulfonamide, and piperidinyl to ...