120979-63-7

Upstream product

• 80089-24-3 benzyl prolinate hydrochloride 
• 16652-71-4 benzyl (2S)-2-pyrrolidinecarboxylate hydrochloride 
• 41036-21-9 (S)-benzyl 1-((R)-2-(tert-butoxycarbonylamino)propanoyl)pyrrolidine-2-carboxylate 
• 118554-12-4 Benzyl N-tert-butyloxycarbonyl-(R,S)-alanyl-(S)-prolinate 

Downstream Products

• 118554-05-5 (S)-1-((R)-2-{N'-[1-(4-Nitro-phenyl)-meth-(E)-ylidene]-hydrazino}-propionyl)-pyrrolidine-2-carboxylic acid benzyl ester 
• 118554-05-5 (S)-1-((S)-2-{N'-[1-(4-Nitro-phenyl)-meth-(E)-ylidene]-hydrazino}-propionyl)-pyrrolidine-2-carboxylic acid benzyl ester 
• 99043-91-1 Boc-D-Tyr(BzlCl₂)-Val-Orn(Z)-Leu-D-Ala-Pro-N₃ 
• 99043-89-7 Boc-D-Tyr(BzlCl₂)-Val-Orn(Z)-Leu-D-Ala-Pro-OBzl 
• 99043-90-0 Boc-D-Tyr(BzlCl₂)-Val-Orn(Z)-Leu-D-Ala-Pro-NHNH₂ 

Relevant academic research and scientific papers

FAP-ACTIVATED THERAPEUTIC AGENTS, AND USES RELATED THERETO

Disclosed are prodrugs of cytotoxic anthracyclines (such as doxorubicin) and other therapeutic agents that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of cytotoxic and other agents to FAP- expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compounds comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer, fibrosis, and inflammation.

FAP-ACTIVATED THERAPEUTIC AGENTS, AND USES RELATED THERETO

Disclosed are prodrugs of anthracyclines (such as doxorubicin) and derivatives thereof that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of "warhead" anthracycline or anthracycline derivative to FAP-expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compounds comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer, undesirable fibrosis, and undesirable inflammation.

A Simple Method for N-Amination of Peptide Derivatives

A smooth and mild procedure is reported for the N-amination of α-amino acid and peptide derivatives with cyclohexanespiro-3'-oxaziridine; the chiral integrity is preserved throughout.