Results 41 to 50 of about 9,016 (186)
Molecules, 2022 In this paper, we report on the design and synthesis of a novel series of quinazoline-2,4(1H,3H)-dione derivatives as fluoroquinolone-like inhibitors of bacterial gyrase and DNA topoisomerase IV to identify and develop antimicrobial agents to prevent ...
Nader M. Boshta +4 more
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Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt
British Journal of Pharmacology, EarlyView.Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown +2 more
wiley +1 more source
circMAN1A2 as an Isoform‐Resolved Circular RNA Hub in Cancer
Cancer Science, EarlyView.circMAN1A2 as an isoform‐resolved circular RNA hub in cancer. circMAN1A2 is generated by back‐splicing of MAN1A2 pre‐mRNA, with alternative circularization producing multiple isoforms, including the predominant circMAN1A2(2–5). Its mechanistic interfaces include miRNA‐associated regulation, RBP binding/proteostasis control, BSJ‐mediated RNA–RNA pairing,
Hanyu Shang +4 more
wiley +1 more source
Sakarya Üniversitesi Fen Bilimleri Enstitüsü Dergisi, 2018 Birçok ülkede olduğu gibi bizimülkemizde de metal korozyonunu önlemeye yönelik kullanılan yöntemlerden biriuygun inhibitör kullanımıdır. Bu amaç doğrultusunda bu çalışmada,4-okso-kinazolin türevi olan uzun karbon zinciri içeren 3 adet katyonikpiridinyum ...
Serkan Öztürk
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Frontiers in Chemistry, 2020 CDK5/p25 kinase plays a major role in neuronal functions, and is hyperactivated in several human cancers including glioblastoma and neurodegenerative pathologies such as Alzheimer's and Parkinson's.
Marion Peyressatre +7 more
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Medicinal Chemistry of Quinazolines as Analgesic and Anti-Inflammatory Agents
ChemEngineering, 2022 Quinazoline is an essential scaffold, known to be linked with various biological activities. Some of the prominent biological activities of this system are analgesic, anti-inflammatory, anti-hypertensive, anti-bacterial, anti-diabetic, anti-malarial ...
Mohamed F. Zayed
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Cell Proliferation, EarlyView.Novel curcumin‐derived M4 binds HSP70's ATPase domain, disrupting HSP70‐mediated lysosomes‐autophagy pathway to inhibit TNBC growth and metastasis, and synergizes with paclitaxel for potent combination therapy. ABSTRACT Structural modification of curcumin yielded a novel series of 1,4‐pentadien‐3‐one oxime ether derivatives, among which compound M4 ...
Zijian Li +6 more
wiley +1 more source
ADAM17 and its proteolytic targets in disease pathogenesis
The FEBS Journal, EarlyView.ADAM17 as a multifunctional sheddase with contrasting roles across inflammatory, metabolic, cardiovascular, and neoplastic diseases. Through regulated activation by iRhom, iTAP/FRMD8, and tetraspanins, ADAM17 cleaves diverse membrane ligands and receptors, thereby promoting inflammation, fibrosis, obesity, insulin resistance, and tumor progression ...
Abdulbasit Amin, Marina Badenes
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Journal of Chemical Research, 2002 The reaction of hydrazones of 2-aminoacetophenone with triphosgene in dichloromethane or benzene in the presence of triethylamine gave quinazolines, pyrazolo[1,5-c]quinazoline and spiro quinazoline dimers. The latter compounds are being reported for the first time.
H. Z. Alkhathlan +4 more
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MoleculesCancer is a complicated, multifaceted disease that can impact any organ in the body. Various chemotherapeutic agents have a low selectivity and are very toxic when used alone or in combination with others.
Heba T. Abdel-Mohsen +4 more
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