193001-91-1Relevant articles and documents
Discovery of a Class of Potent and Selective Non-competitive Sentrin-Specific Protease 1 Inhibitors
Brand, Michael,Frasson, David,Gall, Flavio,Hunziker, Lukas,Kroslakova, Ivana,Lindenmann, Urs,Riedl, Rainer,Sievers, Martin
, (2020/03/24)
Sentrin-specific proteases (SENPs) are responsible for the maturation of small ubiquitin-like modifiers (SUMOs) and the deconjugation of SUMOs from their substrate proteins. Studies on prostate cancer revealed an overexpression of SENP1, which promotes prostate cancer progression as well as metastasis. Therefore, SENP1 has been identified as a novel drug target against prostate cancer. Herein, we report the discovery and biological evaluation of potent and selective SENP1 inhibitors. A structure-activity relationship (SAR) of the newly identified pyridone scaffold revealed allosteric inhibitors with very attractive in vitro ADMET properties regarding plasma binding and plasma stability for this challenging target. This study also emphasizes the importance of biochemical mode of inhibition studies for de novo designed inhibitors.
Tyrosine kinase inhibitors
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, (2008/06/13)
The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
An efficient enantioselective synthesis of (S)-(-)-acromelobic acid
Adamczyk, Maciej,Akireddy, Srinivasa Rao,Reddy, Rajarathnam E.
, p. 3421 - 3423 (2007/10/03)
(Equation Presented) A highly efficient enantioselective synthesis of (S)-(-)-acromelobic acid (1) was achieved via asymmetric hydrogenation of dehydroamino acid derivative (3) using (R,R)-[Rh(DIPAMP)(COD)]BF4 catalyst followed by removal of protective groups in >98% ee and good over all yield. The key intermediate (3) was prepared from the commercially available citrazinic acid (4) in six steps.