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Bioassay-guided fractionation of the CH 2 Cl 2 -soluble extract led to the isolation of 10 compounds. Compounds 8 and 9 reduced the LPS-induced secretion of IL-6 and TNF-α in a RAW264.7 cell line.
Synthesis of a series of substituted 1-aminotetrahydrocarbazoles with potent activity against human papillomaviruses is described. Synthetic approaches allowing for variation of the substitution pattern are outlined and resulting changes in antiviral activity are highlighted.
A series of 3′-aminoflavones 5,6,7,8-tetra or 5,7-dioxygenated on the A-ring was synthesized from tangeretin or naringin, two natural Citrus flavonoids, then evaluated for their antiproliferative and proapoptotic activities, and for the inhibition of tubulin assembly.
A novel compound inhibiting HIV-1 integrase has been identified by means of virtual screening techniques. A small family of structurally related molecules has been synthesized and biologically evaluated with some of the compounds possessing micromolar activity both in enzymatic and cellular assays.
We report the identification of potent and brain-penetrable 2-aminobenzimidazole based MCH1R antagonist 25 .
Peptidomimetic motilin antagonists ( 17c and 17d ) were identified. Both compounds dose-dependently suppressed motilin-induced colonic and gastric motility in conscious dogs.
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