Novel benzofuran-1,3,4-thiadiazole aryl urea hybrids as dual VEGFR-2/BRAF inhibitors: anticancer activity, apoptosis induction, and molecular modeling studies [0.03%]
新型苯并呋喃-1,3,4-噻二唑芳基脲杂化物作为VEGFR-2 / BRAF双重抑制剂：抗肿瘤活性，诱导细胞凋亡和分子建模研究
Marwa I Serag,Mohamed R Elnagar,Wafaa A Ewes et al.
Marwa I Serag et al.
The development of dual-directed anticancer agents has emerged as an effective strategy to simultaneously modulate tumor proliferation and angiogenesis while overcoming resistance associated with single-target therapies. In the present stud...
Design, synthesis and antitubercular evaluation of 2,5-disubstituted 1,3,4-oxadiazoles bearing a 3,5-dinitrophenyl pharmacophore [0.03%]
含3,5-二硝基苯药效团单环三氮唑并[4,3-b]吡啶的合成及抗结核活性研究
Václav Pflégr,Jiřina Stolaříková,Enikő Šikorová et al.
Václav Pflégr et al.
Tuberculosis (TB) continues to demand new chemotypes able to overcome acquired drug-resistance. Here, we designed and synthesized two related series of twenty 3,5-dinitrophenyl-based 1,2-diacylhydrazines and their cyclic analogues, 2,5-disu...
Rational design, synthesis, and evaluation of acridone-peptide based antimicrobial and Antifolate agents against methicilin-resistant Staphylococcus aureus, Bacillus subtilis and dihydrofolate reductase [0.03%]
合理设计、合成及评估抗甲氧西林金黄色葡萄球菌、枯草芽孢杆菌和二氢叶酸还原酶的吖啶酮-肽类抗菌与抗二氢叶酸化合物
Sombir Jaglan,Palwinder Singh,Varinder Kaur et al.
Sombir Jaglan et al.
To conquer the antimicrobial resistance, here, we developed acridone-peptide based DHFR inhibitors. Small peptides or amino acids are coupled with acid acridone either through amide linkage or via an azole-based linker. These hybrids exerte...
Structure-based identification of novel indole-fused polycyclic derivatives as potent acetylcholinesterase inhibitors [0.03%]
基于结构的新型并吲哚多环衍生物作为乙酰胆碱酯酶抑制剂的研究
Wenbin Chen,Keyu Zhan,Chenrui Xu et al.
Wenbin Chen et al.
The pathogenesis of Alzheimer's disease (AD) is closely associated with cholinergic neuronal impairment, which is induced by excessive degradation of acetylcholine (ACh) mediated by acetylcholinesterase (AChE). In this study, a series of no...
One-step selective synthesis of benzofuran or hydroxyacetophenone derivatives with potential anticancer activity [0.03%]
一步选择性合成具有潜在抗肿瘤活性的苯并呋喃或羟基乙酰苯酮衍生物
Ana Maria Birgoanu,Catalina-Ionica Ciobanu,Violeta Mangalagiu et al.
Ana Maria Birgoanu et al.
We present in this work a direct, effective, and selective way to synthesize methylbenzofuran heterocycles or O-alkylated hydroxyacetophenone derivatives, with potential anticancer activity. The reaction pathway is one-step, is thermally co...
A highly selective 1,2-dihydroquinoxaline derivative as a potent PRMT5-MTA complex inhibitor [0.03%]
一种高效的选择性二氢喹唑啉衍生物作为PRMT5-MTA复合物抑制剂
Yiru Liu,Zhihao Jiao,Daoguang Zhang et al.
Yiru Liu et al.
Protein arginine methyltransferase 5 (PRMT5) is a promising therapeutic target in oncology. However, first-generation PRMT5 inhibitors failed in clinical trials due to dose-limiting hematologic toxicity, likely resulting from non-selective ...
Discovery of DA1 as PARP inhibitor for the treatment of BRCA-proficient triple negative breast cancer by suppressing the PI3K/AKT/mTOR signaling pathway [0.03%]
DA1通过抑制PI3K AKT mTOR信号通路用于治疗BRCA阳性三阴性乳腺癌的发现
Yan Qu,Lijie Tang,Song Li et al.
Yan Qu et al.
Currently, PARP inhibitors (PARPis) have been primarily utilized to treat breast cancer susceptibility gene (BRCA)-mutated triple-negative breast cancer (TNBC), but their application scope is quite narrow. Recently, it has been discovered...
Lead optimization of rivastigmine-like hybrids: Impact of nitro group and halogen substitution on multi-target anti-Alzheimer's activity [0.03%]
利伐斯的明类似杂化物的选择优化：硝基及卤素取代物对多靶向抗阿尔茨海默活性的影响
Rosalba Leuci,Marco Paparella,Marco Cerini et al.
Rosalba Leuci et al.
The multifactorial profile of Alzheimer's disease has led researchers to adopt a multi-target strategy for the design of new small molecules. In this context, starting from the structure of ROS151, a novel series of seventeen rivastigmine-l...
Scaffold hopping-directed design and discovery of N1-substituted aminopyrimidine-indole derivatives as FAK inhibitors with anti-pancreatic cancer activity [0.03%]
基于FAK抑制剂的胰腺癌化合物设计与发现研究
Libo Cai,Gang Xu,Shaohua Gou
Libo Cai
Pancreatic cancer, characterized by its highly aggressive malignancy and suboptimal clinical outcomes, remains a formidable global health challenge. Focal adhesion kinase (FAK) functions as a pivotal modulator of diverse cellular pathways, ...
Targeting the NAD+ salvage pathway: Identification of bifunctional NAMPT inhibitors and SIRT1 activators through pharmacophore-based virtual screening [0.03%]
靶向NAD+补救途径：通过药效团虚拟筛选法鉴定双功能NAMPT抑制剂和SIRT1激活剂
Fikriye Ozgencil,Selen Ozge Almamis,Huseyin Cimen et al.
Fikriye Ozgencil et al.
Nicotinamide phosphoribosyltransferase (NAMPT) and Sirtuin 1 (SIRT1) are key regulators of cellular metabolism and NAD+ homeostasis, representing attractive targets in cancer therapy. In this study, we identified novel bifunctional small mo...