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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 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 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...
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 ...
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...
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...
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...