- THIENO[3,2-D]PYRIMIDINE-6-CARBOXAMIDES AND ANALOGUES AS SIRTUIN MODULATORS
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Provided herein are novel substituted thieno[3,2-d]pyrimidine-6-carboxamide sirtuin inhibitors and methods of use thereof. The sirtuin inhibitors may be used for inhibiting a sirtuin-mediated biological process, and, e.g. for treating and/or preventing diseases and disorders including, but not limited to cancer, neurodegenerative disease and inflammation. Also provided herein are pharmaceutical compositions comprising these sirtuin inhibitors and compositions comprising a sirtuin inhibitor in combination with another therapeutic agent.
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Page/Page column 63
(2014/09/29)
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- Discovery of thieno[3,2-d ]pyrimidine-6-carboxamides as potent inhibitors of SIRT1, SIRT2, and SIRT3
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The sirtuins SIRT1, SIRT2, and SIRT3 are NAD+ dependent deacetylases that are considered potential targets for metabolic, inflammatory, oncologic, and neurodegenerative disorders. Encoded library technology (ELT) was used to affinity screen a 1
- Disch, Jeremy S.,Evindar, Ghotas,Chiu, Cynthia H.,Blum, Charles A.,Dai, Han,Jin, Lei,Schuman, Eli,Lind, Kenneth E.,Belyanskaya, Svetlana L.,Deng, Jianghe,Coppo, Frank,Aquilani, Leah,Graybill, Todd L.,Cuozzo, John W.,Lavu, Siva,Mao, Cheney,Vlasuk, George P.,Perni, Robert B.
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p. 3666 - 3679
(2013/06/27)
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