Keywords: تخته سنگ; Sigma 1 receptor (Ï1R); Sigma 2 receptor (Ï2R); Transmembrane protein 97 (TMEM97); Scaffold hopping; Receptor subtype selectivity; Docking;
مقالات ISI تخته سنگ (ترجمه نشده)
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Keywords: تخته سنگ; BM212; Scaffold hopping; Anti-tubercular activity; Microplate alamar blue assay; 2,3-Disubstituted benzimidazoles; 1,2,4-Trisubstituted imidazoles; 2,3-Disubstituted imidazopyridines; Mycobacterium tuberculosis;
Keywords: تخته سنگ; Scaffold hopping; Synthesis; Cannabinoid receptors; CB2 antagonism; ADME model; Docking studies;
Keywords: تخته سنگ; Quinazolinones; Molluscicidal and cercaricidal agents; Structure based drug design; Scaffold hopping; Intramolecular hydrogen bond;
Keywords: تخته سنگ; Migraine; CGRP; Oxazolidinone; Class B GPCR; Scaffold hopping;
Keywords: تخته سنگ; Hedgehog signaling pathway; Smoothened; Antagonist; GPCR; Scaffold hopping; Cancer therapyAUC, area under curve; CE, collision energy; DCM, dichloromethane; DIPEA, N,N-diisopropylethylamine; DMF, N,N-dimethylformamide; DMSO, dimethyl sulfoxide; DP, declus
Keywords: تخته سنگ; Hedgehog pathway; Smoothened; Antagonist; GPCR; Scaffold hopping; Cancer therapy
Discovery of novel 20S proteasome inhibitors by rational topology-based scaffold hopping of bortezomib
Keywords: تخته سنگ; Proteasome inhibitors; Topology-based; Scaffold hopping; Bortezomib;
Discovery of novel CDK inhibitors via scaffold hopping from CAN508
Keywords: تخته سنگ; Pyrazolo[3,4-b]pyridine; Scaffold hopping; CAN508; CDK2; CDK9; Selectivity;
Discovery of EBI-1051: A novel and orally efficacious MEK inhibitor with benzofuran scaffold
Keywords: تخته سنگ; Kinase; MEK inhibitors; Scaffold hopping; Benzofuran;
Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrido[4,3-c]azepin-5-one-based novel chemotype CCR2 antagonists via scaffold hopping strategy
Keywords: تخته سنگ; 6,7,8,9-Tetrahydro-5H-pyrido[43-c]azepin-5-one; 3,4-Dihydro-2,6-naphthyridin-1(2H)-one; CCR2 antagonist; Scaffold hopping; Structure-activity relationship; Selectivity of CCR2 over CCR5;
Scaffold hopping identifies 6,8-disubstituted purines as novel anaplastic lymphoma kinase inhibitors
Keywords: تخته سنگ; ALK; anaplastic lymphoma kinase; cMet; hepatocyte growth factor receptor; DIPEA; N,N-Diisopropylethylamine; DMF; N,N-Dimethylformamide; EML4; echinoderm microtubule-associated protein-like 4; FDA; food and drug administration; gk; gatekeeper; μW; micro w
Potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors based on the benzoisoxazole moiety: application of a bioisosteric scaffold hopping approach to flufenamic acid
Keywords: تخته سنگ; Aldo-keto reductase 1C3; AKR1C3; 17β-HSD5; Prostate cancer (PCa); CRPC; Bioisosterism; Scaffold hopping; Inhibitors; X-ray crystallography;
Design, synthesis, and biological evaluation of novel amide and hydrazide based thioether analogs targeting Histone deacteylase (HDAC) enzymes
Keywords: تخته سنگ; Acrylamide; Hydrazide; Thioether; HDAC; Scaffold hopping;
4-Hydroxy-1,2,3-triazole moiety as bioisostere of the carboxylic acid function: a novel scaffold to probe the orthosteric γ-aminobutyric acid receptor binding site
Keywords: تخته سنگ; Hydroxy-1,2,3-triazole; Bioisosterism; Scaffold hopping; GABAA receptor; GABA; γ-Aminobutyric acid; GABAAR; GABA type A receptor; 4-PIOL; 5-(piperidin-4-yl)-3-isoxazolol; 4-PHP; 4-(piperidin-4-yl)-1-hydroxypyrazole; aza-4-PIOL; 5-(piperidin-4-yl)-3-hydro
Design, synthesis and pharmacological evaluation of N4,N6-disubstituted pyrimidine-4,6-diamine derivatives as potent EGFR inhibitors in non-small cell lung cancer
Keywords: تخته سنگ; EGFR-TKIs; Scaffold hopping; NSCLC;
Discovery and SAR of a novel series of Natriuretic Peptide Receptor-A (NPR-A) agonists
Keywords: تخته سنگ; Natriuretic Peptide Receptor A; Agonist; Scaffold hopping; Thienopyrimidine derivatives; Quinazoline derivatives;
New Caspase-1 inhibitor by scaffold hopping into bio-inspired 3D-fragment space
Keywords: تخته سنگ; Scaffold hopping; 3D fragments; Docking; Natural product; Caspase-1;
Identification of novel PI3K inhibitors through a scaffold hopping strategy
Keywords: تخته سنگ; Scaffold hopping; ETP-46321; PI3K inhibitors; Back-up;
Discovery of furan and dihydrofuran-fused tricyclic benzo[d]imidazole derivatives as potent and orally efficacious microsomal prostaglandin E synthase-1 (mPGES-1) inhibitors: Part-1
Keywords: تخته سنگ; Benzofuran; Prostanoid; Inflammation; Scaffold hopping; Hyperalgesia; PGE2; Osteoarthritis;
Novel hamamelitannin analogues for the treatment of biofilm related MRSA infections-A scaffold hopping approach
Keywords: تخته سنگ; Hamamelitannin analogues; Scaffold hopping; MRSA; Antibiotic potentiators; Quorum sensing;
Discovery of orally bioavailable cyclohexanol-based NR2B-selective NMDA receptor antagonists with analgesic activity utilizing a scaffold hopping approach
Keywords: تخته سنگ; AcOEt; ethyl acetate; chloramine-T; N-chloro 4-methylbenzenesulfonamide sodium salt; DMAP; N,N-4-dimethylaminopyridine; DMF; N,N-dimethylformamide; hERG; human Ether-a-go-go Related Gene; HOBt; 1-hydroxybenzotriazole; IBX; o-iodoxybenzoic acid; LDA; lithi
Hyphenated 3D-QSAR statistical model-scaffold hopping analysis for the identification of potentially potent and selective sigma-2 receptor ligands
Keywords: تخته سنگ; Sigma receptor; Sigma-2 receptor; 3D-QSAR; Scaffold hopping; Virtual screening; Forge and Spark software; Bioisosteric replacements;
Hydroxytriazole derivatives as potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitors discovered by bioisosteric scaffold hopping approach
Keywords: تخته سنگ; Aldo-keto reductase 1C3; AKR1C3; 17β-HSD5; Prostate cancer; CRPC; Bioisosterism; Scaffold hopping; Inhibitors; NWCHXFMRNUJDNB-UHFFFAOYSA-N; HZZCFCAKQYBGLE-UHFFFAOYSA-N; YQJHRNZFIOVGQM-UHFFFAOYSA-N; UHUYUGANTDDPEB-UHFFFAOYSA-N; DWGCYTWMYJCZRX-UHFFFAOYSA-N
Discovery of new chemical entities as potential leads against Mycobacterium tuberculosis
Keywords: تخته سنگ; Anti-tubercular agent; Imidazo[21-b]thiazole; Pyrazolo[51-b]thiazole; Scaffold hopping;
Discovery of EBI-907: A highly potent and orally active B-RafV600E inhibitor for the treatment of melanoma and associated cancers
Keywords: تخته سنگ; B-RafV600E; Kinase; Pyrazolo[3,4-c]isoquinoline; Scaffold hopping; Cancer
Identification of new SUMO activating enzyme 1 inhibitors using virtual screening and scaffold hopping
Keywords: تخته سنگ; Sumoylation; SUMO; SUMO E1 inhibitor; Virtual screening; Scaffold hopping
Discovery of 2-((2-chloro-6-fluorophenyl)amino)-N-(3-fluoro-5-(trifluoromethyl)phenyl)-1-methyl-7,8-dihydro-1H-[1,4]dioxino[2â²,3â²:3,4]benzo[1,2-d]imidazole-5-carboxamide as potent, selective and efficacious microsomal prostaglandin E2 synthase-1 (mPGE
Keywords: تخته سنگ; Rheumatoid arthritis; Benzimidazole; mPGES-1 inhibitor; PGE2; CSF concentration; Scaffold hopping;
Indole-based allosteric inhibitors of HIV-1 integrase
Keywords: تخته سنگ; HIV integrase inhibitor; ALLINI; Scaffold hopping;
Selective CB2 receptor agonists. Part 1: The identification of novel ligands through computer-aided drug design (CADD) approaches
Keywords: تخته سنگ; WWVQOPCDGDSZNA-LBPRGKRZSA-N; ZVPVGKSDCAFJCV-NSHDSACASA-N; WPMZHAWRMPKXHR-ZDUSSCGKSA-NCannabinoid receptor 2; De-novo design; Ligand-based; Scaffold hopping; Proline
Discovery of 4-benzoylamino-N-(prop-2-yn-1-yl)benzamides as novel microRNA-21 inhibitors
Keywords: تخته سنگ; MicroRNA-21; MicroRNA-21 inhibitor; Benzamide; Scaffold hopping
Design and synthesis of a novel series of histamine H3 receptor antagonists through a scaffold hopping strategy
Keywords: تخته سنگ; Histamine H3 receptor antagonist/inverse agonist; Structure activity relationship; Scaffold hopping; Cardiac myocyte model
Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: Development of a potent and CNS penetrant [3.1.0]-based lead
Keywords: تخته سنگ; GlyT1; Scaffold hopping; Transporter; Schizophrenia;
Scaffold hopping of sampangine: Discovery of potent antifungal lead compound against Aspergillus fumigatus and Cryptococcus neoformans
Keywords: تخته سنگ; Sampangine; Scaffold hopping; Antifungal activity;
Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: Development of a [3.3.0]-based series and other piperidine bioisosteres
Keywords: تخته سنگ; GlyT1; Scaffold hopping; Transporter; Schizophrenia;
Scaffold-switching: An exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates
Keywords: تخته سنگ; Antituberculosis; Imidazo[1,2-a]pyridine; Imidazo[1,2-a]pyrimidine; 5,6-Fused bicyclic system; Scaffold hopping;
Scaffold hopping towards potent and selective JAK3 inhibitors: Discovery of novel C-5 substituted pyrrolopyrazines
Keywords: تخته سنگ; Kinase inhibitors; Janus kinase; JAK; Structure based drug design; Scaffold hopping; Intramolecular hydrogen bond;
Synthesis and evaluation of 4-anilinoquinazoline bioisosteres as potential anti-breast cancer agents
Keywords: تخته سنگ; Breast cancer; Cytotoxic activity; Scaffold hopping; Synthesis; ThienopyrimidinesTKIs, tyrosine kinase inhibitors; HER2, human epidermal growth factor receptor 2; EGFR TK, epidermal growth factor receptor tyrosine kinase; EGFR PTK, epidermal growth factor
Design, synthesis, biological evaluation, and comparative docking study of 1,2,4-triazolones as CB1 receptor selective antagonists
Keywords: تخته سنگ; Cannabinoid receptors; Antagonist; 1,2,4-Triazolone; Scaffold hopping; Homology model;
Identification of novel PTP1B inhibitors by pharmacophore based virtual screening, scaffold hopping and docking
Keywords: تخته سنگ; PTP1B inhibitors; Pharmacophore modeling; Scaffold hopping; Docking; Synthesis and biological activity; PTP1B; protein tyrosine phosphatise-1B; QSAR; quantitative structure activity relationship; PBVS; pharmacophore based virtual screening; SAR; structure
Identification of 2-aminooxazole amides as acyl-CoA: Diacylglycerol acyltransferase 1 (DGAT1) inhibitors through scaffold hopping strategy
Keywords: تخته سنگ; DGAT1 inhibitors; Treatment for dyslipidemia; Scaffold hopping;
Novel Mps1 kinase inhibitors: From purine to pyrrolopyrimidine and quinazoline leads
Keywords: تخته سنگ; Mps1; TTK; Protein kinase inhibitors; Scaffold hopping; Conformational restriction; Structure-based design; Cancer; Purines; Pyrrolopyrimidines; Quinazoline;
On scaffold hopping: Challenges in the discovery of sulfated small molecules as mimetics of glycosaminoglycans
Keywords: تخته سنگ; Allosteric inhibition; Anticoagulants; Scaffold hopping; Thrombin; Virtual screening;
Imidazo[4,5-b]pyridine inhibitors of B-Raf kinase
Keywords: تخته سنگ; B-Raf; Imidazopyridine; Scaffold hopping; DFG-in; αC-helix out;
Discovery of novel PTP1B inhibitors via pharmacophore-oriented scaffold hopping from Ertiprotafib
Keywords: تخته سنگ; PTP1B inhibitors; Pharmacophore; Scaffold hopping; Ertiprotafib;
Scaffold hopping approach towards various AFQ-056 analogs as potent metabotropic glutamate receptor 5 negative allosteric modulators
Keywords: تخته سنگ; CIZDIEPYKQXGQG-UHFFFAOYSA-N; OFNVYYXEOJUGRH-UHFFFAOYSA-N; SONLNLJEFBMKGV-UHFFFAOYSA-N; Metabotropic glutamate receptor; mGluR5; Allosteric modulator; Scaffold hopping; AFQ-056;
Scaffold-hopping strategy toward calanolides with nitrogen-containing heterocycles
Keywords: تخته سنگ; Calanolides; Scaffold hopping; Nitrogen-containing heterocycles
Design and synthesis of novel benzoheterocyclic derivatives as human acrosin inhibitors by scaffold hopping
Keywords: تخته سنگ; 3-Phenylisoxazole; Scaffold hopping; Synthesis; Molecular docking; Human acrosin inhibitors
Database of bioactive ring systems with calculated properties and its use in bioisosteric design and scaffold hopping
Keywords: تخته سنگ; Cheminformatics; Bioisosteric design; Scaffold; Scaffold hopping; Scaffold properties; Bioisosteric search;
Hit to lead evaluation of 1,2,3-triazolo[4,5-b]pyridines as PIM kinase inhibitors
Keywords: تخته سنگ; PIM inhibitors; Scaffold hopping; Triazolopyridine; Hit to lead; Phosphorylation of BAD; FLT-3; Crystal structure; Docking; hERG Binding; Mechanism of action