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We report the syntheses and evaluation of amidinobenzofuran derivatives as tryptase inhibitors. Among the compounds we evaluated, 1,5-Bis(4-(5-amidinobenzofuran-2-ylcarbonyl)piperazinylcarbonylmethoxy)cyclooctane 26 (AY0068) was found to be a selective and potent non-peptide inhibitor. 26 was...
The design and syntheses of non-thiol inhibitors of farnesyl-protein transferase are described. Optimization of cysteine-substituted diarylethers led to highly potent imidazole-containing diarylethers and diarylsulfones. Polar diaryl linkers dramatically improved potency and gave highly cell...
A series of N -phenylalkyl-substituted tropane analogs of boat conformation was synthesized, and these tropanes were evaluated for their ability to inhibit high affinity uptake of dopamine (DA) and serotonin (5-HT) into striatal nerve endings (synaptosomes). Some of these compounds exhibit high...
Dicarba- closo -dodecaboranes (carboranes), which have spherical geometry and hydrophobicity, are applicable as a hydrophobic pharmacophore of biologically active molecules. We have investigated structure-activity relations based on the structure of the potent estrogenic agonist,...
While two structurally related epoxyketone-containing antitumor natural products, epoxomicin and eponemycin, share the proteasome as a common intracellular target, they differ in their antiproliferative activity, proteasome subunit binding specificity, and rates of proteasome inhibition. As a...
The chemical structure and bioactivity of phomalairdenone ( 7 ), a new sesquiterpenic host-selective phytotoxin produced by an unusual virulent type isolate of the blackleg fungus ( Phoma lingam , perfect stage Leptosphaeria maculans (Desm.) Ces. et de Not.) are reported.
In the course of a study of 6- N -amino-substituted analogues of NB-506 ( 1 ), a more potent anticancer drug, J-109,404 ( 2 ), in which the formyl group of NB-506 was replaced with a 1,3-dihydroxypropane group, was reported. A study of further modification in the positions of two hydroxyl groups...
Seventeen aporphines were tested for antiplatelet activity. L-(+)-hernovine HCl and 7-hydroxydehydrothalicsimidine strongly inhibited platelet aggregation induced by adenosine 5′-diphosphate (ADP), arachidonic acid (AA), collagen, and platelet-activating factor (PAF). The latter showed the...
The benzothiophene LY329146 reverses the drug resistance phenotype in multidrug resistance protein (MRP1)-overexpressing cells when dosed in combination with MRP1-associated oncolytics doxorubicin and vincristine. Additionally, LY329146 inhibited MRP1-mediated uptake of the MRP1 substrate LTC 4...
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