Within the last year
Within the past 3 years
1 - 10 of 25 articles
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...
Save this article to read later. You can see your Read Later on your DeepDyve homepage.
To save an article, log in first, or sign up for a DeepDyve account if you don't already have one.
Sign Up Log In
To subscribe to email alerts, please log in first, or sign up for a DeepDyve account if you don't already have one.
Read and print from thousands of top scholarly journals.
Sign up with Facebook
Sign up with Google
Already have an account? Log in
To get new article updates from a journal on your personalized homepage, please log in first, or sign up for a DeepDyve account if you don't already have one.