159857-88-2

Upstream product

• 3397-32-8 N-(benzyloxycarbonyl)-phenylalanine-N-hydroxysuccinimide ester 
• 501-53-1 benzyl chloroformate 
• 1161-13-3 N-Cbz-L-Phe 
• 63-91-2 L-phenylalanine 
• 56-87-1 L-lysine 
• 6298-03-9 (2S)-2-amino-6-{[(prop-2-en-1-yloxy)carbonyl]amino}hexanoic acid 

Downstream Products

• 159857-89-3 N-Cbz-Phe-Lys(ε-Alloc)-4-aminobenzyl alcohol 
• 1279111-08-8 Benzyloxycarbonyl-L-phenylalanyl-L-lysyl-PABC-deacetylcolchicine 
• 1279111-09-9 Benzyloxycarbonyl-L-phenylalanyl-L-lysyl-PABC-4-fluorodeacetylcolchicine 
• 1279111-12-4 C₅₅H₆₀FN₅O₁₃ 
• 1279111-11-3 C₅₅H₆₁N₅O₁₃ 
• 71448-16-3 Cbz-L-Phe-L-Lys-OH 
• 159857-90-6 N-Cbz-Phe-Lys(ε-Alloc)-4-aminobenzyl 4-nitrophenyl carbonate 

Relevant academic research and scientific papers

CONJUGATE COMPOUNDS

The invention relates to sphingoglycolipid analogues and peptide derivatives thereof, which are useful in treating or preventing diseases or such as those relating to infection, atopic disorders, autoimmune diseases or cancer.

Design, synthesis, and antitumor activity of 4-halocolchicines and their pro-drugs activated by cathepsin B

Novel colchicine derivatives possessing various substituents at the C4 position were prepared. Among them, 4-halo derivatives 3-6 were found to exhibit higher activity against cancer cell lines (A549, HT29, HCT116) as well as on mice transplanted with the HCT116 human colorectal carcinoma cell line than colchicine (1). Further, utilizing the 4-substituted colchicines, we prepared pro-drugs having a dipeptide side chain and demonstrated that these pro-drugs were activated by cathepsin B, an enzyme overexpressed in tumor cells, and exhibited selective toxicity to the tumor cells.

Cathepsin B-sensitive dipeptide prodrugs. 1. A model study of structural requirements for efficient release of doxorubicin

A series of lysosomal protease-sensitive peptides attached to doxorubicin (DOX) was prepared as model substrates for internalizing anticancer immunoconjugates and potential antimetastasis prodrugs. Rates of cathepsin B-mediated release of free drug was measured for each, and human plasma stabilities for representative examples.