61294-22-2Relevant academic research and scientific papers
MODIFIED PROTEINS AND PROTEIN DEGRADERS
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, (2021/12/08)
Provided herein are compounds, pharmaceutical compositions, and methods for binding or degrading target proteins. Further provided herein are compounds having a DNA damage-binding protein 1 (DDB1) binding moiety. Some such embodiments include a linker. Some such embodiments include a target protein binding moiety. Further provided herein are ligand-DDB1 complexes. Further provided herein are in vivo modified DDB1 proteins.
Design, synthesis and biological evaluation of hybrid nitroxide-based non-steroidal anti-inflammatory drugs
Thomas, Komba,Moody, Terry W.,Jensen, Robert T.,Tong, Jason,Rayner, Cassie L.,Barnett, Nigel L.,Fairfull-Smith, Kathryn E.,Ridnour, Lisa A.,Wink, David A.,Bottle, Steven E.
, p. 34 - 47 (2018/02/09)
Dual-acting hybrid anti-oxidant/anti-inflammatory agents were developed employing the principle of pharmacophore hybridization. Hybrid agents were synthesized by combining stable anti-oxidant nitroxides with conventional non-steroidal anti-inflammatory drugs (NSAIDs). Several of the hybrid nitroxide-NSAID conjugates displayed promising anti-oxidant and anti-inflammatory effects on two Non-Small Cell Lung Cancer (NSCLC) cells (A549 and NCI-H1299) and in ameliorating oxidative stress induced in 661 W retinal cells. One ester-linked nitroxide-aspirin analogue (27) delivered better anti-inflammatory effects (cyclooxygenase inhibition) than the parent compound (aspirin), and also showed similar reactive oxygen scavenging activity to the anti-oxidant, Tempol. In addition, a nitroxide linked to the anti-inflammatory drug indomethacin (39) significantly ameliorated the effects of oxidative stress on 661 W retinal neurons at efficacies greater or equal to the anti-oxidant Lutein. Other examples of the hybrid conjugates displayed promising anti-cancer activity, as demonstrated by their inhibitory effects on the proliferation of A549 NSCLC cells.
Antiulcer effect of the N- and 0-β-D-glucopyranosides of 5- aminosalicylic acid
Sztaricskai, Ferenc,Takacs, Ildiko E.,Pusztai, Ferenc,Szabo, Gabor,Csipo, Istvan
, p. 321 - 326 (2007/10/03)
Starting from methyl 5-nitrosalicylate (20) the N- and O-β- glucopyranosyl derivatives (24, 28) of 5-aminosalicylic acid were prepared. The LD50 values of these compounds were determined on mice, and the inhibitory effect of 24 (0.83 mmol/kg) and 28 (1.2 mmol/kg) on gastric ulcer on rats, induced by indomethacin was investigated.
Protease inhibitors
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, (2008/06/13)
This invention relates to methods of preventing or reducing the degradation of elastin and other proteins and thereby preventing or retarding the disease states caused by said degradation by administering compounds, some of which are novel, of the formula: STR1 or their pharmacologically acceptable salts.
