Small Molecules Inspired by the Natural Product Withanolides as Potent Inhibitors of Wnt Signaling
Sign Up to like & getrecommendations! Published in 2017 at "ChemBioChem"
DOI: 10.1002/cbic.201700260
Abstract: Wnt signaling is a fundamental pathway that drives embryonic development and is essential for stem cell maintenance and tissue homeostasis. Dysregulation of Wnt signaling is linked to various diseases, and a constitutively active Wnt pathway… read more here.
Keywords: wnt signaling; small molecules; inhibitors wnt; natural product ... See more keywords
Exploration of Zinc(II) Complexes as Potent Inhibitors Against Protein Tyrosine Phosphatase 1B
Sign Up to like & getrecommendations! Published in 2019 at "Chemical Research in Chinese Universities"
DOI: 10.1007/s40242-019-8265-8
Abstract: Although protein tyrosine phosphatases(PTPs) do not contain any metals, their activities can be inhibited by some metal complexes. Here we investigated the inhibition of two zinc complexes with Schiff base ligands against PTPs activity to… read more here.
Keywords: phosphatase; tyrosine phosphatase; zinc complexes; protein tyrosine ... See more keywords
Potent inhibitors of human LAT1 (SLC7A5) transporter based on dithiazole and dithiazine compounds for development of anticancer drugs.
Sign Up to like & getrecommendations! Published in 2017 at "Biochemical pharmacology"
DOI: 10.1016/j.bcp.2017.07.006
Abstract: The LAT1 transporter is acknowledged as a pharmacological target of tumours since it is strongly overexpressed in many human cancers. The purpose of this work was to find novel compounds exhibiting potent and prolonged inhibition… read more here.
Keywords: based dithiazole; inhibition; dithiazole dithiazine; potent inhibitors ... See more keywords
New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.111573
Abstract: The carbonic anhydrase (CA) inhibitory activity of newly synthesized compounds 4-21 against the human CA (hCA) isoforms I, II, IX, and XII was measured and compared to that of standard sulfonamide inhibitors, acetazolamide (AAZ) and… read more here.
Keywords: new anthranilic; 0111 kis; slc 0111; aaz slc ... See more keywords
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b00929
Abstract: On the basis of our earlier discovery of N1-selective inhibitors, the 150-cavity of influenza virus neuraminidases (NAs) could be further exploited to yield more potent oseltamivir derivatives. Among the synthesized compounds, 15b and 15c were… read more here.
Keywords: substituted oseltamivir; oseltamivir derivatives; derivatives potent; group ... See more keywords
Potent Inhibitors of Thioredoxin Glutathione Reductase: Grail of Anti-Schistosome Drug within Reach?
Sign Up to like & getrecommendations! Published in 2020 at "ACS infectious diseases"
DOI: 10.1021/acsinfecdis.0c00072
Abstract: Species of the blood fluke Schistosoma are responsible for schistosomiasis, the second most common parasitic disease, which is prevalent particularly in poor communities. Under redox pressure, schistosomes survive in mammalian hosts with the help of… read more here.
Keywords: thioredoxin glutathione; inhibitors thioredoxin; glutathione reductase; drug ... See more keywords
Bioactive phytoconstituents as potent inhibitors of casein kinase-2: dual implications in cancer and COVID-19 therapeutics
Sign Up to like & getrecommendations! Published in 2022 at "RSC Advances"
DOI: 10.1039/d1ra09339h
Abstract: Casein kinase 2 (CK2) is a conserved serine/threonine-protein kinase involved in hematopoietic cell survival, cell cycle control, DNA repair, and other cellular processes. It plays a significant role in cancer progression and viral infection. CK2… read more here.
Keywords: inhibitors casein; phytoconstituents potent; potent inhibitors; casein kinase ... See more keywords
Homology modeling of human GABA-AT and devise some novel and potent inhibitors via computer-aided drug design techniques
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Biomolecular Structure and Dynamics"
DOI: 10.1080/07391102.2020.1774417
Abstract: Abstract γ-aminobutyric acid aminotransferase (GABA-AT) is a pyridoxal 5′-phosphate (PLP)-dependent enzyme which degrades γ-aminobutyric (GABA) in the brain. GABA is an important inhibitory neurotransmitter that plays important neurological roles in the brain. Therefore, GABA-AT is… read more here.
Keywords: novel potent; drug; devise novel; gaba ... See more keywords
An Enhanced Hybrid Screening Approach to Identify Potent Inhibitors for the SARS-CoV-2 Main Protease From the NCI Compound Library
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Chemistry"
DOI: 10.3389/fchem.2022.816576
Abstract: The emergence and rapid spread of SARS-CoV-2, the pathogen of COVID-19, have caused a worldwide public health crisis. The SARS-CoV-2 main protease (Mpro) is an essential enzyme for the virus and therefore an appealing target… read more here.
Keywords: sars cov; screening; potent inhibitors; cov main ... See more keywords
Monosubstituted Acetophenone Thiosemicarbazones as Potent Inhibitors of Tyrosinase: Synthesis, Inhibitory Studies, and Molecular Docking
Sign Up to like & getrecommendations! Published in 2021 at "Pharmaceuticals"
DOI: 10.3390/ph14010074
Abstract: A set of 12 monosubstituted acetophenone thiosemicarbazone derivatives (TSCs) were synthesized and their inhibitory properties toward tyrosinase activity were tested. Moreover, their ability to inhibit melanogenesis in the B16F10 murine melanoma cell line was studied.… read more here.
Keywords: inhibitory; monosubstituted acetophenone; potent inhibitors; molecular docking ... See more keywords