The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.6b01496
Abstract: Current pain therapeutics suffer from undesirable psychotropic and sedative side effects, as well as abuse potential. Glycine receptors (GlyRs) are inhibitory ligand-gated ion channels expressed in nerves of the spinal dorsal horn, where their activation… read more here.
Keywords: tricyclic sulfonamides; lead optimization; glycine receptors; optimization ... See more keywords
Human Estrogen Receptor Alpha Antagonists, Part 3: 3-D Pharmacophore and 3-D QSAR Guided Brefeldin A Hit-to-Lead Optimization toward New Breast Cancer Suppressants
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DOI: 10.3390/molecules27092823
Abstract: The estrogen receptor α (ERα) is an important biological target mediating 17β-estradiol driven breast cancer (BC) development. Aiming to develop innovative drugs against BC, either wild-type or mutated ligand-ERα complexes were used as source data… read more here.
Keywords: hit lead; estrogen receptor; breast cancer; pharmacophore qsar ... See more keywords
On drug discovery against infectious diseases and academic medicinal chemistry contributions
Sign Up to like & getrecommendations! Published in 2022 at "Beilstein Journal of Organic Chemistry"
DOI: 10.3762/bjoc.18.141
Abstract: This perspective is an attempt to document the problems that medicinal chemists are facing in drug discovery. It is also trying to identify relevant/possible, research areas in which academics can have an impact and should… read more here.
Keywords: hit lead; drug discovery; medicinal chemistry; academic medicinal ... See more keywords