Expanding the tetrazole space: medicinal chemistry, biological diversity and structure-activity relationships [0.03%]
扩大四氮唑空间:药物化学、生物多样性和构效关系
Anuradha Singampalli,Pardeep Kumar,Rani Bandela et al.
Anuradha Singampalli et al.
Tetrazole, a synthetic five-membered heterocycle composed of one carbon and four nitrogen atoms, has emerged as a privileged scaffold in modern drug discovery. Despite its absence in natural products, the tetrazole ring is widely recognized...
Thiazolidin-based dual Aurora kinase inhibitors with potent anticancer activity [0.03%]
一类具有高效抗肿瘤活性的噻唑啶类 aurora 激酶双靶点抑制剂
Walid E Elgammal,Hazem Elkady,Aisha A Alsfouk et al.
Walid E Elgammal et al.
Aims: To design, synthesize, and evaluate novel thiazolidin derivatives as potential dual inhibitors of Aurora kinases for anticancer therapy. Materials a...
Indole-based kinase modulators for NSCLC: recent advances in synthetic route, SAR and molecular docking studies [0.03%]
基于吲哚的激酶调节剂在非小细胞肺癌中的最新研究进展:合成路线、结构活性关系和分子对接研究
Shivam Nag,Divyanshi Thakur,Kalicharan Sharma
Shivam Nag
Aim: The indole scaffold has gained increasing importance due to its structural versatility and ability to interact with multiple cancerous receptors relevant to non-small cell lung cancer (NSCLC). So, the aim of this rev...
Urease inhibitors: current advances, therapeutic potentials, and clinical challenges [0.03%]
脲酶抑制剂:目前的研究进展、治疗潜力及临床挑战
Omer Habis Alzoubi,Almuatasim Khamees,Mohammad Basil Alzubi et al.
Omer Habis Alzoubi et al.
Urease is a nickel-dependent metalloenzyme that catalyzes urea hydrolysis, generating ammonia and elevating local pH, a process implicated in the pathogenesis of Helicobacter pylori-associated peptic ulcer disease (PUD). To identify effecti...
Butenolide-based human carbonic anhydrase (hCA) I/II inhibitors: integrated computational and biological evaluation [0.03%]
基于人的碳酸酐酶(hCA)I/II抑制剂的丁内酯:计算和生物学综合评价
Songul Bayrak,Cansu Ozturk,Serpil Gerni et al.
Songul Bayrak et al.
Aims: This study aimed to evaluate the inhibitory effects of a series of butenolide derivatives on human carbonic anhydrase isoenzymes I and II (hCA I and hCA II) and to investigate their antioxidant and antimicrobial pro...
Sandeep Kumar,Vijay Kumar Bhat
Sandeep Kumar
Aims: This study aims to analyze the molecular structures of anticancer drugs using graph-theoretic parameters and to investigate their structural properties through metric-based descriptors. ...
Investigation of the in silico, in vitro, and in vivo effects of a novel amino acid conjugate against DMBA-induced breast cancer in rats [0.03%]
一种新型氨基酸缀合物对大鼠二甲基苯并蒽诱导的乳腺癌的体内和体外研究
Muhammed Ismail Can,Abdullah Aslan,Kenan Koran et al.
Muhammed Ismail Can et al.
This study aims to perform molecular docking analyses of a newly synthesized candidate compound and to investigate its therapeutic efficacy in vivo at an appropriate dose in a female rat model with induced breast cancer. To this end, the Cy...
Synthesis, biological profiling, and computational investigation of 1,2,4-triazole-5-thione-quinoline Schiff base hybrids [0.03%]
含1,2,4-三氮唑-5-硫杂异喹啉席夫碱衍生物的合成、活性筛选及分子机制研究
Ergün Gültekin,Hacer Doğan,Abdurrahman Atalay et al.
Ergün Gültekin et al.
Aims: To synthesize novel 1,2,4-triazole-5-thione-quinoline Schiff base hybrids and evaluate their urease inhibitory, antimicrobial, antioxidant, and computational properties. ...
Novel isoxazole-(thio-) and semicarbazone hybrids as promising antibacterial and anticancer agents: synthesis, characterization, biological evaluation, and in silico validation [0.03%]
具有抗菌和抗肿瘤作用的新型异噁唑-(硫)-和半 carbazone 杂化物:合成,表征,生物评估和计算机模拟验证
Muneera S M Al-Saleem,Jehan Y Al-Humaidi,Abd Elaziz Rahhou et al.
Muneera S M Al-Saleem et al.
Aims: This study aims to design and synthesize a new series of hybrid heterocyclic systems and to evaluate their anticancer and antimicrobial properties. Additionally, in silico analyses were performed to assess their mol...
Recent advances in the development of EGFR/Src, Src/Abl, EGFR/VEGFR2, EGFR/c-Met, STAT-3/c-Src, VGERF/FAK and EGFR/HER dual-targeted kinase inhibitors [0.03%]
近年开发的EGFR/Src、Src/Abl、EGFR/VEGFR2、EGFR/c-Met、STAT-3/c-Src、VEGF/FAK和EGFR/HER双靶向激酶抑制剂研究进展
Eman Bobtaina,Sureyya Olgen
Eman Bobtaina
Introduction: Although several therapies have been applied for cancer treatment and mutations, drug resistance remains a significant impediment to the efficient use of single-therapy. Multi-targeting therapies are designe...