200283-08-5

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 111-41-1 2-(2-Aminoethylamino)ethanol 
• 208577-84-8 [2-(2-Hydroxy-ethylamino)-ethyl]-carbamic acid tert-butyl ester 

Downstream Products

• 200283-09-6 N-(O-(3-maleinimidobenzoyl)-2-hydroxyethyl)-N,N'-bis-tertiarybutyloxycarbonyl-1,2-diaminoethane 
• 554-68-7 triethylamine hydrochloride 
• 120131-72-8 N-(2-aminoethyl)-N-[2-[[(1,1-dimethylethoxy)carbonyl]amino]ethyl]carbamate-1,1-dimethylethyl ester 

Relevant academic research and scientific papers

Convenient synthesis of a galacturonic acid based macrocycle with potential copper-complexation ability

A convenient approach to the construction of a galacturonic acid based macrocycle containing an amide group and a triazole ring has been achieved. The key step relies on the efficient formation of a 16-membered ring by a copper-catalysed intramolecular cycloaddition reaction applied to analkyne-azide galacturonate. Depending on the reaction conditions, the outcome of the 1,3-dipolar cycloaddition varied; the expected intramolecular 1,4-triazole was obtained as well as a C2-symmetric dimer in different ratios. A preliminary study of the complexation properties of this macrocycle towards CuII cations revealed the formation of cryptates in a 1:1 metal/ligand ratio. A galacturonic acid based macrocycle containing an amide group and a triazole ring has been synthesized by a procedure involving a copper-catalysed intramolecular cycloaddition reaction as the key step. The results of a preliminary study of the complexation properties of this macrocycle towards CuII cations are described. Copyright

Traceable platinum(II) complexes with alkylene diamine-derived ligands: synthesis, characterization and in vitro studies

Diiodido- (6a/6b) and dichloridoplatinum(II) complexes (7a/7b) with fluorescent ligands 2-[(2-aminoethyl)amino]ethyl-2-(methylamino)benzoate (5a) and 2-amino-1-(aminoethyl)ethyl-2-(methylamino)benzoate (5b) were prepared and characterized by elemental ana

COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS

The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.

ANTIBACTERIAL BASIC BIAROMATIC DERIVATIVES WITH AMINOALKOXY SUBSTITUTION

The invention relates to antibacterial compounds of formula I wherein R1a, R2a, R2b, R3a, R3b, R4, R5, U1, U2, U3, U4, V1, V2, V3, V4, X and Q and n are as defined in the specification. It further relates pharmaceutical compositions containing these compounds and the uses of these compounds in the manufacture of medicaments for the treatment of bacterial infections. These compounds are useful antimicrobial agents effective against a variety of human and veterinary pathogens including among others Gram-positive and Gram-negative aerobic and anaerobic bacteria.

MACROCYCLIC TGF-BR2 KINASE INHIBITORS

The present invention relates to macrocyclic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of Transforming Growth Factor beta Receptor 2 (TGF-β R2) and/or mutants thereof, for use in the diag

Inhibitors of DNA Methyltransferase

The invention relates to the inhibition of DNA methyltransferase isoforms DNMT1 and DNMT3b2. The invention provides compounds and methods for inhibiting DNMT1 and DNMT3b2.

Tagging (arene)ruthenium(II) anticancer complexes with fluorescent labels

Fluorescent (arene)ruthenium(II) complexes have been prepared by tagging a small fluorogenic reporter onto the chelating ligand of complexes of the type [(η6-arene)RuCl(Z)]+ (Z = chelating ligand). Complexes [(η6-p-cym)-Ru

Design, Synthesis, and Biological Evaluation of Indenoisoquinoline Topoisomerase I Inhibitors Featuring Polyamine Side Chains on the Lactam Nitrogen

The indenoisoquinolines are a class of noncamptothecin topoisomerase I inhibitors that display significant cytotoxicity in human cancer cell cultures. They offer a number of potential advantages over the camptothecins, including greater chemical stability, formation of more persistent cleavage complexes, and induction of a unique pattern of DNA cleavage sites. Molecular modeling has suggested that substituents on the indenoisoquinoline lactam nitrogen would protrude out of the DNA duplex in the ternary cleavage complex through the major groove. This indicates that relatively large substituents in that location would be tolerated without compromising biological activity. As a strategy for increasing the potencies and potential therapeutic usefulness of the indenoisoquinolines, a series of compounds was synthesized containing polyamine side chains on the lactam nitrogen. The rationale for the synthesis of these compounds was that the positively charged ammonium cations would increase DNA affinity through electrostatic binding to the negatively charged DNA backbone, and the polyamines might also facilitate cellular uptake by utilization of polyamine transporters. The key step in the synthesis involved the condensation of Schiff bases, containing protected amine side chains, with substituted homophthalic anhydrides, to afford cis-3-aryl-4-carboxy-1-isoquinolones. These isoquinolones were then converted to indenoisoquinolines with thionyl chloride. Although monoamines were much more potent than the lead compound, no significant increase in potency was observed through incorporation of additional amino groups in the side chain. However, one of the monoamine analogues, which features a bis(2-hydroxyethyl)amino group in the side chain, proved to be one of the most cytotoxic indenoisoquinoline synthesized to date, with a GI50 mean-graph midpoint (MGM) of 0.07 μM in the NIH human cancer cell culture screen, and topoisomerase I inhibitory activity comparable to that of camptothecin.