22509-74-6Relevant articles and documents
Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors
Blackledge, Chuck W.,Bonnette, William,Burgess, Joelle,Carson, Jeffrey D.,Creasy, Caretha L.,Elkins, Patricia,Graves, Alan P.,Heerding, Dirk A.,Knapp-Reed, Beth,Kruger, Ryan,Luengo, Juan,McHugh, Charles,Mohammad, Helai,Nagarajan, Raman,Pappalardi, Melissa Baker,Qu, Junya,Reif, Alexander,Schulz, Mark,Stern, Melissa,Su, Dai-Shi,Wang, Liping,Wong, Kristen,Yu, Hongyi,Zeng, Jenny
supporting information, (2020/02/06)
We report herein the discovery of isoxazole amides as potent and selective SET and MYND Domain-Containing Protein 3 (SMYD3) inhibitors. Elucidation of the structure-activity relationship of the high-throughput screening (HTS) lead compound 1 provided potent and selective SMYD3 inhibitors. The SAR optimization, cocrystal structures of small molecules with SMYD3, and mode of inhibition (MOI) characterization of compounds are described. The synthesis and biological and pharmacokinetic profiles of compounds are also presented.
COMBINATION THERAPIES WITH IRE1 SMALL MOLECULE INHIBITORS
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Paragraph 00288, (2020/12/01)
Provided herein are methods of using IRE1 small molecule inhibitors in combination therapies for treating cancer in a subject. The IRE1 small molecule inhibitors described herein may be used in combination therapies for treating solid and hematologic cancers.
Synthesis and application of peptide borate compounds
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Paragraph 0111-0114, (2019/12/25)
The invention belongs to the field of drug synthesis, and specifically relates to a series of novel peptide borate compounds or pharmaceutical salts thereof, and a preparation method and pharmaceutical application thereof. The structure of the peptide borate compounds or the pharmaceutical salts thereof is as shown in a formula I which is described in the specification. The compounds of the invention can be used for preparing proteasome inhibitors, and thus can be further used for treating solid tumors and blood tumors.