Spirooxindol‐1,3‐oxazine Alkaloids: Highly Potent and Selective Antitumor Agents Evolved from Iterative Structure Optimization
Sign Up to like & getrecommendations! Published in 2022 at "Chemmedchem"
DOI: 10.1002/cmdc.202200162
Abstract: Spirooxindole‐1,3‐oxazines are a small and structurally unique class of spirooxindole alkaloids. To date, only four of these compounds have been isolated from natural sources, and their biological properties remained unknown thus far. Dioxyreserpine is a… read more here.
Keywords: highly potent; oxazine alkaloids; spirooxindol oxazine; alkaloids highly ... See more keywords
Discovery of novel cholic acid derivatives as highly potent agonists for G protein-coupled bile acid receptor.
Sign Up to like & getrecommendations! Published in 2021 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2021.105588
Abstract: In this study, fourteen new cholic acid (CA) derivatives were designed and synthesized, and the GloSensor cAMP accumulation assay indicated that all derivatives could activate the Takeda G protein-coupled receptor 5 (TGR5). Methylation of 7-… read more here.
Keywords: cholic acid; acid; protein coupled; highly potent ... See more keywords
Discovery of highly potent human glutaminyl cyclase (QC) inhibitors as anti-Alzheimer's agents by the combination of pharmacophore-based and structure-based design.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113819
Abstract: The inhibition of glutaminyl cyclase (QC) may provide a promising strategy for the treatment of early Alzheimer's disease (AD) by reducing the amount of the toxic pyroform of β-amyloid (AβΝ3pE) in the brains of AD… read more here.
Keywords: glutaminyl cyclase; highly potent; potent human; cyclase ... See more keywords
Novel, highly potent and in vivo active inhibitor of GABA transporter subtype 1 with anticonvulsant, anxiolytic, antidepressant and antinociceptive properties
Sign Up to like & getrecommendations! Published in 2017 at "Neuropharmacology"
DOI: 10.1016/j.neuropharm.2016.10.019
Abstract: Background and purpose: Since GABAergic dysfunction underlies a variety of neurological and psychiatric disorders, numerous strategies leading to the augmentation of GABAergic neurotransmission have been introduced. One of them is the inhibition of GABA reuptake… read more here.
Keywords: highly potent; ddpm 2571; inhibitor; antidepressant ... See more keywords
An enveloped virus-like particle vaccine expressing a stabilized prefusion form of the SARS-CoV-2 spike protein elicits highly potent immunity
Sign Up to like & getrecommendations! Published in 2021 at "Vaccine"
DOI: 10.1016/j.vaccine.2021.07.034
Abstract: We evaluated enveloped virus-like particles (eVLPs) expressing various forms of the Severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) spike protein and several adjuvants in an effort to identify a highly potent Coronavirus disease 2019 (COVID-19) vaccine… read more here.
Keywords: highly potent; vaccine; cov spike; spike protein ... See more keywords
Rational Design of Highly Potent, Selective, and Bioavailable SGK1 Protein Kinase Inhibitors for the Treatment of Osteoarthritis.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01601
Abstract: The serine/threonine kinase SGK1 is an activator of the β-catenin pathway and a powerful stimulator of cartilage degradation that is found to be upregulated under genomic control in diseased osteoarthritic cartilage. Today, no oral disease-modifying… read more here.
Keywords: sgk1; highly potent; treatment; rational design ... See more keywords
Discovery of a Highly Potent and Selective Dual PROTAC Degrader of CDK12 and CDK13
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.2c00384
Abstract: Selective degradation of the cyclin-dependent kinases 12 and 13 (CDK12/13) presents a novel therapeutic opportunity for triple-negative breast cancer (TNBC), but there is still a lack of dual CDK12/13 degraders. Here, we report the discovery… read more here.
Keywords: cdk12; highly potent; cdk12 cdk13; selective dual ... See more keywords
Discovery of SPH3127: A Novel, Highly Potent, and Orally Active Direct Renin Inhibitor.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00834
Abstract: Renin is the rate-limiting enzyme in the renin-angiotensin-aldosterone system (RAAS) which regulates blood pressure and renal function and hence is an attractive target for the treatment of hypertension and cardiovascular/renal diseases. However, the development of… read more here.
Keywords: highly potent; direct renin; novel highly; discovery sph3127 ... See more keywords
The Highly Potent AhR Agonist Picoberin Modulates Hh-Dependent Osteoblast Differentiation
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.2c00956
Abstract: Identification and analysis of small molecule bioactivity in target-agnostic cellular assays and monitoring changes in phenotype followed by identification of the biological target are a powerful approach for the identification of novel bioactive chemical matter… read more here.
Keywords: highly potent; potent ahr; ahr agonist; identification ... See more keywords
Development of a Highly Potent Transthyretin Amyloidogenesis Inhibitor: Design, Synthesis, and Evaluation
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.2c01195
Abstract: Transthyretin amyloidosis (ATTR) is a group of fatal diseases described by the misfolding and amyloid deposition of transthyretin (TTR). Discovering small molecules that bind and stabilize the TTR tetramer, preventing its dissociation and subsequent aggregation,… read more here.
Keywords: highly potent; development highly; design; transthyretin amyloidogenesis ... See more keywords
Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b01709
Abstract: The emergence of drug-resistant HIV from a widespread antiviral chemotherapy targeting HIV protease in the past decades is unavoidable and provides a challenge to develop alternative inhibitors. We synthesized a series of allophenylnorstatine-based peptidomimetics with… read more here.
Keywords: highly potent; protease; type protease; allophenylnorstatine based ... See more keywords