201541-51-7

Upstream product

• 201006-25-9 tert-butyl (S)-5-(3-(4-methoxy-2,3,6-trimethylphenylsulfonyl)guanidino)-1-oxo-1-(thiazol-2-yl)pentan-2-ylcarbamate 
• 102185-38-6 Nα-(t-butyloxycarbonyl)-Nω-(4-methoxy-2,3,6-trimethylbenzenesulphonyl)-L-arginine 
• 142801-55-6 N-α-(t-butyloxycarbonyl)-N'-ω'-(4-methoxy-2,3,6-trimethylbenzenesulfonyl)-L-arginine-N,O-dimethylhydroxyamide 

Downstream Products

• 894147-76-3 C₃₂H₄₂N₆O₇S₂ 

Relevant academic research and scientific papers

Structure-based design, synthesis, and biological evaluation of Leu-Arg dipeptide analogs as novel hepsin inhibitors

Hepsin, a type II transmembrane serine protease, is an attractive protein as a potential therapeutic and diagnostic biomarker for prostate cancer because it is highly up-regulated in prostate cancer and promotes both progression and metastasis. Starting from the reported tetrapeptide hepsin inhibitor Ac-KQLR-ketothiazole (kt) (1), we investigated the minimal structural requirements for hepsin inhibitory activity by truncating amino acids at the N-terminus. The kt and ketobenzothiazole (kbt) dipeptide analogs Ac-LR-kt (3) and Ac-LR-kbt (15) were found to be potent hepsin inhibitors, exhibiting Ki values of 22 nM and 3 nM, respectively. The present work suggests that LR-containing dipeptide molecules could be useful as lead compounds for the development of novel hepsin inhibitors.

INHIBITORS OF GROWTH FACTOR ACTIVATION ENZYMES

The present invention generally relates to compounds that are useful for inhibiting one or more of hepatocyte growth factor activator, matriptase, hepsin, Factor Xa, or thrombin. The present invention also relates to various methods of using the inhibitor compounds including treating a malignancy, a pre-malignant condition, or cancer by administering an effective amount of the inhibitor to a subject in need thereof.

Inhibitors of HGFA, matriptase, and hepsin serine proteases: A nonkinase strategy to block cell signaling in cancer

Hepatocyte growth factor activators (HGFA), matriptase, and hepsin are S1 family trypsin-like serine proteases. These proteases proteolytically cleave the single-chain zymogen precursors, pro-HGF (hepatocyte growth factor), and pro-MSP (macrophage stimula

Synthesis, SAR exploration, and X-ray crystal structures of factor XIa inhibitors containing an α-ketothiazole arginine

Using an α-ketothiazole arginine moiety as a key recognition element, a series of small peptidomimetic molecules was designed and synthesized, and their co-crystal structures with factor XIa were studied in an effort to develop smaller, less peptidic inhibitors as antithrombotic agents.

Process for the preparation of chiral keto-heterocycles of basic amino acids

A process for the preparation of novel keto heterocycle derivatives of basic natural and unnatural amino acids which affords products of high enantiomeric excess where a metalated heterocycle is reacted with N,O-dialkyl amide of an amino acid containing arylsulphonamide protected side chain amine in high chemical and optical yield as well as the novel compounds obtained by the process.

Pyrrolo[1,2-a]pyrazine-1,4-dione serine protease inhibitors

PCT No. PCT/US97/09832 Sec. 371 Date Oct. 27, 1998 Sec. 102(e) Date Oct. 27, 1998 PCT Filed Jun. 10, 1997 PCT Pub. No. WO97/48706 PCT Pub. Date Dec. 24, 1997This invention relates to pyrrolo[1,2-a]pyrazine-1,4-diones of general formula: wherein B is carbonyl or methylene, R2, R4, R5, and R6 are hydrogen, alkyl, or substituted alkyl, A is a basic group, and Q is hydrogen or a keto heterocycle group. The compounds are inhibitors of serine proteases, typically thrombin, Factor Xa, and Factor VIIa, and are useful for treating and preventing thrombotic disorders.