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Design and synthesis of novel arylurea derivatives of aryloxy(1-phenylpropyl) alicyclic diamines with antimicrobial activity against multidrug-resistant Gram-positive bacteria
KeywordsArylurea derivativesAntibacterial propertiesAnti-MRSA activityAnti-VRE activityAnti-LRSE activityDepolarization of...
Design, synthesis, and repurposing of O6-aminoalkyl-sulfuretin analogs towards discovery of potential lead compounds as antileishmanial agents
Up to date, there are still significantly unmet clinical needs for treatment of the fatal visceral leishmaniasis; a neglec...
Designed switch from covalent to non-covalent inhibitors of carboxylesterase Notum activity
N-Acyl indolines 4 are potent, non-covalent Notum inhibitors developed from a covalent virtual screening hit 2a. The lead ...
Discovery of acridine-based LSD1 inhibitors as immune activators targeting LSD1 in gastric cancer
LSD1 is overexpressed in various cancers and promotes tumor cell proliferation, tumor expansion, and suppresses immune cel...
Discovery of novel benzamide derivatives bearing benzamidophenyl and phenylacetamidophenyl scaffolds as potential antitumor agents via targeting PARP-1
Poly(ADP-ribose) polymerase-1 (PARP-1) plays a crucial role in DNA damage repair and has been identified as a promising th...
Discovery of 3,5-diaryl-1H-pyrazol-based ureas as potent RET inhibitors
Rearranged during transfection (RET) is a promising target for antitumor drug development. Multikinase inhibitors (MKI) ha...
Optimization of carbazole carboxamide RORγt agonists: Challenges in improving the metabolic stability and maintaining the agonistic activity
Based on two previously discovered carbazole carboxamide retinoic acid receptor-related orphan receptor-γt (RORγt) agonist...
Optimization of triazolo[4,5-d]pyrimidines towards human CC chemokine receptor 7 (CCR7) antagonists
CCR7 signaling directs the migration of both immune cells and cancer cells to the lymph nodes, is involved in numerous chr...
C-glycosides analogues of the okadaic acid central fragment exert neuroprotection via restoration of PP2A-phosphatase activity: A rational design of potential drugs for Alzheimer's disease targeting tauopathies
Protein phosphatase 2A (PP2A) is an important Ser/Thr phosphatase that participates in the regulation of multiple cellular...
A practical “preTACs-cytoblot” platform accelerates the streamlined development of PROTAC-based protein degraders
With the growing importance of PROTAC-mediated protein degradation in drug discovery, robust synthetic methodologies and r...
Optically activated MEK1/2 inhibitors (Opti-MEKi) as potential antimelanoma agents
Mitogen-activated protein kinase kinases 1/2 (MEK1/2) play critical roles in the canonicalRAS/RAF/MEK/ERK pathway. Highly ...
Design, synthesis and biological evaluation of Nucleosidic CD99 inhibitors that selectively reduce Ewing sarcoma viability
Ewing Sarcoma (ES) is a cancer of bone and soft tissues affecting mostly children and young adults. Aggressive progression...
Discovery of phenylcarbamoyl xanthone derivatives as potent neuroprotective agents for treating ischemic stroke
Compounds of natural sources are widespread discovered in the treatment of ischemic stroke. Alpha-mangostin, a natural pre...
Antitumor effect of 3-(quinolin-2-ylmethylene)-4,6-dimethyl-5-hydroxy-7-azaoxindole down-regulating the Gas6-Axl axis
In this study, a new series of 3-arylidene-4,6-dimethyl-5-hydroxy-7-azaoxindole compounds with a wide range of functional ...
Development of the “hidden” multi-target-directed ligands by AChE/BuChE for the treatment of Alzheimer's disease
Accumulation of evidences suggested that excessive amounts of AChE and BuChE in the brain of AD patients at the different ...
3,4-Dihydrobenzo[e][1,2,3]oxathiazine 2,2-dioxide analogs act as potential AMPA receptor potentiators with antidepressant activity
Major depressive disorder is a common psychiatric disorder, with ∼30% of patients suffering from treatment-resistant depre...
Discovery of a novel 1H-pyrazole- [3,4-b] pyridine-based lysine demethylase 5B inhibitor with potential anti-prostate cancer activity that perturbs the phosphoinositide 3-kinase/AKT pathway
Lysine demethylase 5B (KDM5B) is a member of the Jumonji AT-rich interactive domain 1 family. Its main function is to deme...
Novel pyridinium cationic pleuromutilin analogues overcoming bacterial multidrug resistance
A series of pyridinium cation-substituted pleuromutilin analogues were designed, synthesized and evaluated for their antib...
Synthesis and preclinical evaluation of a heterodimeric radioligand targeting fibroblast activation protein and integrin-αvβ3
Tumor progression is accompanied by intrinsic heterogeneity and different phenotypes, which implies a different expression...
Discovery of orally effective and safe GPR40 agonists by incorporating a chiral, rigid and polar sulfoxide into β-position to the carboxylic acid
KeywordsGPR40Glucose-stimulated insulin secretionType 2 diabetes mellitusLipophilicityLiver safetyThree-in-one pharmacopho...
RSK inhibitors as potential anticancer agents: Discovery, optimization, and challenges
Ribosomal S6 kinase (RSK) family is a group of serine/threonine kinases, including four isoforms (RSK1/2/3/4). As a downst...
From PROTAC to inhibitor: Structure-guided discovery of potent and orally bioavailable BET inhibitors
An X-ray structure of a CLICK chemistry-based BET PROTAC bound to BRD2(BD2) inspired synthesis of JQ1 derived heterocyclic...
From lead to clinic: A review of the structural design of P2X7R antagonists
P2X7R, which is a member of the purinergic P2 receptor family, is widely expressed in many immune cells, such as macrophag...
Recent updates on 1,2,3-triazole-containing hybrids with in vivo therapeutic potential against cancers: A mini-review
1,2,3-Triazole moiety which is usually constructed by highly versatile, efficacious and selective copper-catalyzed azide-a...
N-sulfonyl peptide-hybrids as a new class of dengue virus protease inhibitors
KeywordsDengueFlavivirusNS2B-NS3 proteaseSulfonamideN-Sulfonyl peptide-hybridsInChIKeysRRCPKVCUBZNZRY-KKUQBAQOSA-NRLQAKSNV...
Design, synthesis, and biological evaluation of novel dihydropteridone derivatives possessing oxadiazoles moiety as potent inhibitors of PLK1
Polo like kinase 1 (PLK1) is a serine/threonine kinase that is widely distributed in eukaryotic cells and plays an importa...
Korupensamine A, but not its atropisomer, korupensamine B, inhibits SARS-CoV-2 in vitro by targeting its main protease (Mpro)
By combining docking and molecular dynamics simulations, we explored a library of 65 mostly axially chiral naphthylisoquin...
Specific discrimination and efficient elimination of gram-positive bacteria by an aggregation-induced emission-active ruthenium (II) photosensitizer
The infections caused by Gram-positive bacteria (G+) have seriously endangered public heath due to their high morbidity an...
Recent advances of mitochondrial complex I inhibitors for cancer therapy: Current status and future perspectives
Mitochondrial complex I (CI) as a critical multifunctional respiratory complex of electron transport chain (ETC) in mitoch...
Discovery of a novel oral type Ⅰ CDK8 inhibitor against acute myeloid leukemia
CDK8 plays a key role in acute myeloid leukemia, colorectal cancer and other cancers. Here, a total of 54 compounds were d...
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