نتایج جستجو برای: chemotype
تعداد نتایج: 584 فیلتر نتایج به سال:
The fast pace of drug discovery programs, aided by highthroughput screening campaigns, often relies on the generation of combinatorial libraries to identify new chemical entities. The Ugi 4and 3-component reactions in particular [1], have proven to be robust in producing both tool compounds and drugs [2,3]. Here we report a high-throughput entry into the imidazopyridine scaffold, using a microf...
Gatorbulin-1, a distinct cyclodepsipeptide chemotype, targets a seventh tubulin pharmacological site
Significance Natural products provide the inspiration for most drugs, and marine natural products, in particular, are emerging as promising new therapeutics with targets or mechanisms of action. Pharmacological targeting tubulin dynamics has been a validated strategy cancer therapy decades, yielding structurally diverse derivatives, including paclitaxel, vincristine, maytansine, eribulin, six k...
Biophysical fragment screening of a thermostabilized β1-adrenergic receptor (β1AR) using surface plasmon resonance (SPR) enabled the identification of moderate affinity, high ligand efficiency (LE) arylpiperazine hits 7 and 8. Subsequent hit to lead follow-up confirmed the activity of the chemotype, and a structure-based design approach using protein-ligand crystal structures of the β1AR result...
Five new pregnane-type steroids, sclerosteroids J-N (1-5), and a diterpenoid with a new chemotype 3-methyl-5-(10'-acetoxy-2',6',10'-trimethylundecyl)-2-penten-5-olide (6), have been isolated from a soft coral Scleronephthya gracillimum. The structures of the metabolites were determined by extensive spectroscopic analysis. Compound 4 exhibited cytotoxicity against HepG2, A549, and MDA-MB-231 can...
Further purification of the apolar extracts of the sponge Plakinastrella mamillaris, afforded a new oxygenated polyketide named gracilioether K, together with the previously isolated gracilioethers E-G and gracilioethers I and J. The structure of the new compound has been elucidated by extensive NMR (1H and 13C, COSY, HSQC, HMBC, and ROESY) and ESI-MS analysis. With the exception of gracilioeth...
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