501005-45-4

Upstream product

• 870-46-2 t-butoxycarbonylhydrazine 
• 5437-45-6 Benzyl bromoacetate 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 609366-54-3 benzyl [N,N,N'-tris(tert-butyloxycarbonyl)hydrazino]acetate 
• 339201-27-3 N-amino-N-tert-butyloxycarbonylglycine benzyl ester 
• 261380-41-0 [N,N,N'-tris(tert-butyloxycarbonyl)hydrazino]acetic acid 

Relevant academic research and scientific papers

Solid-phase functionalization of peptides by an α-hydrazinoacetyl group

A novel procedure for the preparation of α-hydrazinoacetyl peptides is reported on the basis of the solid-phase coupling of partially or fully Boc-protected hydrazinoacetic acid derivatives. The degree of unwanted polymerization of the activated ester dur

Diazaborines Are a Versatile Platform to Develop ROS-Responsive Antibody Drug Conjugates**

Antibody–drug conjugates (ADCs) are a new class of therapeutics that combine the lethality of potent cytotoxic drugs with the targeting ability of antibodies to selectively deliver drugs to cancer cells. In this study we show for the first time the synthesis of a reactive-oxygen-species (ROS)-responsive ADC (VL-DAB31-SN-38) that is highly selective and cytotoxic to B-cell lymphoma (CLBL-1 cell line, IC50 value of 54.1 nM). The synthesis of this ADC was possible due to the discovery that diazaborines (DABs) are a very effective ROS-responsive unit that are also very stable in buffer and in plasma. DFT calculations performed on this system revealed a favorable energetic profile (ΔGR=?74.3 kcal mol?1) similar to the oxidation mechanism of aromatic boronic acids. DABs’ very fast formation rate and modularity enabled the construction of different ROS-responsive linkers featuring self-immolative modules, bioorthogonal functions, and bioconjugation handles. These structures were used in the site-selective functionalization of a VL antibody domain and in the construction of the homogeneous ADC.

TUNABLE PROBES FOR SELECTIVE PROTEIN LABELLING AND ENZYME INHIBITION

The present invention relates to methods of selectively reacting a compound of Formula (I) with a cysteine residue, which is contained in the sequence of a polypeptide. The methods may be employed in the fields of labelling polypeptides, detecting polypep

NOVEL AZAPEPTIDE OR AZAPEPTIDOMIMETIC COMPOUNDS INHIBITING BCRP AND/OR P-GP

The present invention relates to compounds of azapeptide or azapeptidomimetic type of formula (I): in which R1, R2, R3, X1, X2, X3, X4 and Y are as defined in claim 1, to pharmaceutical compositions containing them and to such compounds as adjuvant for an anticancer or anti-infectious medicament.

Design, synthesis and cardioprotective effect of a new class of dual-acting agents: Phenolic tetrahydro-β-carboline RGD peptidomimetic conjugates

In this study, a new class of phenolic tetrahydro-β-carboline RGD peptidomimetic conjugates was designed and synthesized. The radical scavenging activities of these newly synthesized compounds 12a-c were evaluated in PC12 cell survival assays. The NO scav

Solid-phase synthesis of "mixed" peptidomimetics using Fmoc-protected aza-β3-amino acids and α-amino acids

A solid-phase fluorenylmethyloxycarbonyl (Fmoc)-based synthesis strategy is described for "mixed" aza-β3-peptides as well as a convenient general approach for their required building blocks, the aza-β3-amino acid residues (aza-β3-aa). These monomers allow the synthesis of relatively large quantities of pure mixed aza-β3-peptides. The required Fmoc-substituted aza-β3-amino acids are accessible by convenient synthesis, and a number of monomers including those containing side chains with functional groups have been synthesized. The method was applied toward the solid-phase ynthesis of aza-β3-peptide mimetics of a biologically active histone H4 sequence.