Kebreab Ghebreselasie

TL;DR: These conjugates are important tools for the elucidation of the direct influence of COX inhibitors on platinum‐based anticancer drugs in tumor cells and seem to facilitate cellular accumulation of the platinum drugs and thus improve the efficacy of the antitumor agents.

TL;DR: The results indicate that 2-AG is readily converted to 1(3)-AG under conditions commonly used to study receptor-ligand interactions, findings that have significant implications for the interpretation of relative ligand potency between the two isomers.

TL;DR: Structures reveal that the oxicams bind to the active site of COX-2 using a binding pose not seen with other NSAIDs through two highly coordinated water molecules.

TL;DR: The SAR study revealed that indomethacin conjugates are the best COX-2-targeted agents compared to the other carboxylic acid-containing nonsteroidal anti-inflammatory drugs (NSAIDs) or COX2-selective inhibitors (COXIBs), and an n-butyldiamide linker is optimal for tethering bulky fluorescent functionalities onto the NSAID or COxIB cores.

TL;DR: The in vitro and in vivo properties of compound 7 suggest it will be a useful probe for early detection of cancer and for evaluation of the COX-2 status of premalignant and malignant tumors.