159857-63-3

Upstream product

• 101214-43-1 Fmoc-Phe-ONSu 
• 159857-61-1 (S)-2-amino-6-((4-methoxyphenyl)diphenylmethyl-amino)hexanoic acid 
• 159857-60-0 Fmoc-Lys(Mmt)-OH 
• 623-04-1 4-aminobenzenemethanol 
• 159857-62-2 Fmoc-Phe-Lys(MMT) 
• 450366-22-0 Fmoc-Lys(Mmt)-aminobenzyl alcohol 

Downstream Products

• 159857-65-5 MC-Phe-Lys(MMT)-PAB-OH 
• 159857-66-6 Carbonic acid 4-((S)-2-{(S)-2-[6-(2,5-dioxo-2,5-dihydro-pyrrol-1-yl)-hexanoylamino]-3-phenyl-propionylamino}-6-{[(4-methoxy-phenyl)-diphenyl-methyl]-amino}-hexanoylamino)-benzyl ester 4-nitro-phenyl ester 
• 159857-64-4 (S)-2-((S)-2-amino-3-phenyl-propionylamino)-6-{[(4-methoxy-phenyl)-diphenyl-methyl]-amino}-hexanoic acid (4-hydroxymethyl-phenyl)-amide 

Relevant academic research and scientific papers

Synthesis of an immunoconjugate of camptothecin

The first immunoconjugate of camptothecin has been synthesized wherein the drug is attached to the tumor-recognizing antibody BR96 via a Cathepsin B cleavable linker. Endocytosis of the immunoconjugate upon binding to the tumor cell followed by enzymatic cleavage of the linker inside the endosome ensures tumor-specific release of the drug. In this way, it is hoped that the dose-limiting side effects associated with camptothecin can be eliminated while the antitumor activity is preserved.

POLYCONJUGATES FOR DELIVERY OF RNAI TRIGGERS TO TUMOR CELLS IN VIVO

The present invention is directed compositions for delivery of RNA interference (RNAi) triggers to integrin positive tumor cells in vivo. The compositions comprise RGD ligand- targeted amphipathic membrane active polyamines reversibly modified with enzyme cleavable dipeptide-amidobenzyl-carbonate masking agents. Modification masks membrane activity of the polymer while reversibility provides physiological responsiveness. The reversibly modified polyamines (dynamic polyconjugate or conjugate) are further covalently linked to an RNAi trigger.

Cobalamin conjugates for anti-tumor therapy

The present invention provides a cobalamin-drug conjugate suitable for the treatment of tumor related diseases. Cobalamin is indirectly covalently bound to an anti-tumor drug via a cleavable linker and one or more optional spacers. Cobalamin is covalently

Monomethoxytrityl (MMT) as a versatile amino protecting group for complex prodrugs of anticancer compounds sensitive to strong acids, bases and nucleophiles

Cathepsin B-sensitive maleimidocaproyl-Phe-Lys linker compounds containing acid-sensitive anticancer drugs doxorubicin, mitomycin C and paclitaxel (taxol) attached through a self-immolative p-aminobenzylcarbonyl spacer were prepared using monomethoxytrityl (MMT) as the amino protecting group for Lys. MMT could be removed cleanly and in high yield by dichloroacetic and chloroacetic acids in the presence of anisole with minimal workup.