84110-34-9Relevant articles and documents
Synthesis of four isotopically labeled forms of a proteasome inhibitor, bortezomib
Li, Yuexian,Plesescu, Mihaela,Sheehan, Patrick,Daniels, J. Scott,Prakash, Shimoga R.
, p. 402 - 406 (2007)
[D2](1R)-3-methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(pyrazinylcarbonyl) amino]propyl]-amino]butyl] boronic acid ([D2]bortezomib), a proteasome inhibitor, was synthesized in 11 steps from isobutyryl chloride. Key steps in the synthesis inclu
SUBSTITUTED BORIC ACID COMPOUND, PHARMACEUTICAL COMPOSITION COMPRISING SAME, AND APPLICATION THEREOF
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Paragraph 0038; 0041, (2019/05/10)
A substituted boric acid compound, a pharmaceutical composition comprising same, and an application thereof. The substituted boric acid compound is a compound represented by formula (I), or a crystal form, a pharmaceutically acceptable salt, a prodrug, a stereoisomer, a hydrate, or a solvent compound thereof. The boric acid compound has proteasome inhibitory activity, good pharmacodynamic/pharmacokinetic performance, good applicability, and high safety, and can be used for preparing drugs for treating diseases related to proteasomes.
De Novo Design of Boron-Based Peptidomimetics as Potent Inhibitors of Human ClpP in the Presence of Human ClpX
Tan, Joanne,Grouleff, Julie J.,Jitkova, Yulia,Diaz, Diego B.,Griffith, Elizabeth C.,Shao, Wenjie,Bogdanchikova, Anastasia F.,Poda, Gennady,Schimmer, Aaron D.,Lee, Richard E.,Yudin, Andrei K.
, p. 6377 - 6390 (2019/08/02)
Boronic acids have attracted the attention of synthetic and medicinal chemists due to boron's ability to modulate enzyme function. Recently, we demonstrated that boron-containing amphoteric building blocks facilitate the discovery of bioactive aminoboronic acids. Herein, we have augmented this capability with a de novo library design and a virtual screening platform modified for covalent ligands. This technique has allowed us to rapidly design and identify a series of α-aminoboronic acids as the first inhibitors of human ClpXP, which is responsible for the degradation of misfolded proteins.