157893-14-6Relevant articles and documents
Synthesis of novel benzbromarone derivatives designed to avoid metabolic activation
Ohe, Tomoyuki,Umezawa, Ryutaro,Kitagawara, Yumina,Yasuda, Daisuke,Takahashi, Kyoko,Nakamura, Shigeo,Abe, Akiko,Sekine, Shuichi,Ito, Kousei,Okunushi, Kentaro,Morio, Hanae,Furihata, Tomomi,Anzai, Naohiko,Mashino, Tadahiko
supporting information, p. 3708 - 3711 (2018/11/02)
We synthesized six novel BBR derivatives that were designed to avoid metabolic activation via ipso-substitution and evaluated for their degree of toxicity and hURAT1 inhibition. It was found that all of the derivatives demonstrate lower cytotoxicity in mouse hepatocytes and lower levels of metabolic activation than BBR, while maintaining their inhibitory activity toward the uric acid transporter. We propose that these derivatives could serve as effective uricosuric agents that have much better safety profiles than BBR.
COMBINATION THERAPIES FOR TREATMENT OF CANCER
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, (2016/04/09)
Combination therapies for treatment of cancers associated with mutations in the KRAS gene are provided. Compositions comprising therapeutic agents for treatment of cancers associated with mutations in the KRAS gene are also provided.
COVALENT INHIBITORS OF KRAS G12C
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, (2014/09/30)
Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.