Exploring the Role of Novel N (4) Substituted 5,7-Dibromoisatin Thiosemicarbazones in Modulating PTOV1 Activity for Therapeutic Relevance in Breast Cancer [0.03%]
探究新型N（4）取代的5,7-二溴异丁香硫半卡巴肼调节PTOV1活性以用于乳腺癌治疗的相关性研究
Piyush Kumar,Upendra Chaudhary,Kuldeep Mahiya et al.
Piyush Kumar et al.
We herein report the synthesis, and antiproliferative evaluation of a novel series of N(4)-substituted 5,7-dibromoisatin thiosemicarbazones (TSCs). Structure and activity based approach was used to synthesize derivatives: N(4)-pyrrolidinyl ...
Structure-Guided Design and Mechanistic Elucidation of New Chromene Derivatives as Selective Vascular Endothelial Growth Factor Receptor-2 Inhibitors With Potent Anticancer Activity [0.03%]
基于结构设计及新香豆素衍生物作为选择性血管内皮生长因子受体-2抑制剂的抗肿瘤活性研究
Hazem Elkady,Walid E Elgammal,Ibrahim H Eissa et al.
Hazem Elkady et al.
In this study, a novel series of chromene-based derivatives was rationally designed as potential VEGFR-2 inhibitors based on key structural and pharmacophoric features required for antiangiogenic activity. Accordingly, twelve chromene deriv...
Antitumor Activity of Sodium Selenite, Palbociclib, and Disulfiram Against Osteosarcoma and Rhabdomyosarcoma Cell Lines [0.03%]
亚硒酸钠、Palbociclib和断硫醇对骨肉瘤和横纹肌肉瘤细胞系的抗肿瘤活性
María Ángeles Chico,Kevin Doello,Raul Ortiz et al.
María Ángeles Chico et al.
Osteosarcoma and rhabdomyosarcoma are the most common pediatric sarcomas, yet prognosis remains poor due to high relapse rates. This study investigates the repurposing of palbociclib (PB) and disulfiram (DS), alongside sodium selenite (SS),...
Design, Synthesis, Biological Evaluation, and Molecular Modeling Studies of Novel 2-Aminothiazole Derivatives as Potential FOXM1 Inhibitors for Triple-Negative Breast Cancer Therapy and Structure-Activity Relationship [0.03%]
设计、合成、生物评价及分子模拟研究：新型2-氨基噻唑类化合物作为三阴性乳腺癌治疗的FOXM1抑制剂及构效关系研究
Khaled A N Abusharkh,Venhar Çınar,Alper Onder et al.
Khaled A N Abusharkh et al.
Triple Negative Breast Cancer (TNBC) is one of the most aggressive subtypes of breast cancer (BC), which is associated with a very poor prognosis. It is a broad category of tumors with a variety of biological, clinical, and morphological ch...
Design, Green Synthesis, and Biological Evaluation of Novel Triaryl-Tethered Acryloyl Derivatives as New Generation β-Tubulin Inhibitors for Hepatocellular Carcinoma Treatment [0.03%]
新型三芳基连接丙烯酰衍生物的设计、绿色合成及作为下一代β-微管蛋白抑制剂治疗肝细胞癌的生物学评价研究
Aamal A Al-Mutairi,Mai A E Mourad,Arwa Sultan Alqahtani et al.
Aamal A Al-Mutairi et al.
Inhibition of β-tubulin polymerization has been set as promising therapeutic strategy for cancer therapy. Accordingly, a new set of triaryl-tethered acetohydrazide-acryloyl derivatives were designed and synthesized. The antiproliferative i...
The Development of Chemical Probes for Targeting Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitors [0.03%]
针对辅激活蛋白相关精氨酸甲基转移酶1(CARM1)抑制剂的化学探针的发展
Kadalipura P Rakesh,Santosh Kumar Verma,Man Vir Singh et al.
Kadalipura P Rakesh et al.
As a transcriptional coactivator and associated arginine methyltransferase 1, CARM1 controls various biological functions. CARM1 was thought to be a prospective therapeutic target, as anomalous appearance of the gene has been linked to the ...
Sustained DNA Hypomethylation Induced by a DNA Methyltransferase 1 Inhibitor Triggers Apoptosis in Thyroid Cancer Cells [0.03%]
DNA甲基转移酶1抑制剂诱导甲状腺癌细胞DNA低甲基化并引发细胞凋亡
Chao-Wen Cheng,Wen-Fang Fang,Yuan-Hung Wang et al.
Chao-Wen Cheng et al.
DNA methylation, is catalyzed by DNA methyltransferases (DNMTs), and its aberrant patterns are implicated in thyroid cancer pathogenesis. The study aimed to investigate the association of DNMTs with thyroid cancer and evaluated the effects ...
Discovery of Tetrahydropyrrolo[3,4-c]pyrrole-1,3-dione Derivatives as Novel RIPK1 Inhibitors via Pharmacophore-Based Virtual Screening [0.03%]
基于药效团的虚拟筛选发现新型RIPK1抑制剂四氢吡咯并吡啶-1,3-二酮衍生物
Xin Zeng,Yanzhen Yu,Yifan Wu et al.
Xin Zeng et al.
RIPK1 regulates the pathways in programmed cell death, and is closely associated with inflammatory and immune diseases. Based on the pharmacophore-based virtual screening, compound 15, a tetrahydropyrrolo[3,4-c]pyrrole-1,3-dione derivative,...
FDA-Approved Drugs Containing D-Amino Acids: A Historical and Developmental Perspective [0.03%]
从历史发展角度分析含有D型氨基酸的美国食品药品管理局批准药物状况
Linh Tran,Tien Dung Nguyen,Abdelrahman Gamil Gad et al.
Linh Tran et al.
d-Amino acids, the non-natural enantiomers of l-amino acids, have emerged as powerful tools in peptide drug development due to their unique biochemical properties. Their resistance to proteolytic degradation, enhanced conformational rigidit...
Vitexicarpin Directly Targets RSK2 to Attenuate Migration and Invasion of Triple-Negative Breast Cancer Through Modulating HIF-1α/MMP-9 Pathway [0.03%]
激活素A通过ACVR1/SMAD2信号促进三阴性乳腺癌迁移和侵袭作用的研究及伏邪承气汤的干预作用研究
Shuhui You,Tianhui Wu,Min Qian et al.
Shuhui You et al.
Triple-negative breast cancer (TNBC) is an aggressive subtype of breast cancer with high metastatic potential and lacking effective treatment strategies. Vitexicarpin (VIT) has been reported to have excellent inhibitory effects on several t...