51992-85-9Relevant academic research and scientific papers
Synthesis and evaluation of a class of 1,4,7-triazacyclononane derivatives as iron depletion antitumor agents
Wang, Sheng,Gai, Yongkang,Zhang, Shasha,Ke, Lei,Ma, Xiang,Xiang, Guangya
, p. 117 - 121 (2018)
Iron depletion has been confirmed as an efficient strategy for cancer treatment. In the current study, a series of 1,4,7-triazacyclononane derivatives HE-NO2A, HP-NO2A and NE2P2A, as well as the bifunctional chelators p-NO2-PhPr-NE3TA and p-NH
Controlling multivalency and multimodality: Up to pentamodal dendritic platforms based on diethylenetriaminepentaacetic acid cores
Pulido, Daniel,Albericio, Fernando,Royo, Miriam
supporting information, p. 1318 - 1321 (2014/04/03)
A highly versatile synthetic strategy is described to generate multimodal and multivalent platforms based on a diethylenetriaminepentaacetic (DTPA) core. Compounds with different functionalization patterns, from mono- to pentamodal, have been prepared using robust and simple chemistry.
Stable aziridinium salts as versatile intermediates: Isolation and regio- and stereoselective ring-opening and rearrangement
Song, Hyun A.,Dadwal, Mamta,Lee, Yeseul,Mick, Emily,Chong, Hyun-Soon
supporting information; scheme or table, p. 1328 - 1330 (2009/06/30)
Rock trapping and exploration: Aziridinium bromide salts were discovered serendipitously during bromination of N,N-dicarboxymethylated β-amino alcohols. Regiospecific ring-opening and rearrangement of the isolated, surprisingly stable aziridinium salts produces useful molecules including C-functionalized oxomorpholines and α,β-unsaturated amines. 2009 Wiley-VCH Verleg GmbH & Co. KGaA, Weinheim.
Efficient synthesis and evaluation of bimodal ligand NETA
Chong, Hyun-Soon,Song, Hyun A.,Birch, Noah,Le, Thien,Lim, Sooyoun,Ma, Xiang
supporting information; experimental part, p. 3436 - 3439 (2009/04/11)
The efficient and short synthetic route to the structurally novel bimodal ligand NETA for antibody-targeted radiation therapy (radioimmunotherapy, RIT) of cancer was developed. The structure of NETA was determined by X-ray crystallography. The arsenazo-ba
Tumor-targeted optical contrast agents
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Page 9, (2010/02/07)
Cyanine dye bioconjugates useful for diagnostic imaging and therapy are disclosed. The conjugates include several cyanine dyes with a variety of bis- and tetrakis (carboxylic acid) homologs. The compounds may be conjugated to bioactive peptides, carbohydr
Synthesis of Enantiomerically Pure Diethylenetriaminepentaacetic Acid Analogues. L-Phenylalanine as the Educt for Substitution at the Central Acetic Acid
Williams, Matthew A.,Rapoport, Henry
, p. 1151 - 1158 (2007/10/02)
The enantiospecific synthesis of diethylenetriaminepentaacetic acid (DTPA) analogues from L-phenylalanine via a bis N-alkylation strategy is described.N-Alkylation of p-nitrophenylalanine benzyl ester (4) occurs readily with dibenzyl and di-tert-butyl diacetates 5a and 5b using a phosphate buffer/acetonitrile reaction medium.N,N-Dialkyl (2a,2b) and N-monoalkyl (3a,3b) derivatives of L-p-nitrophenylalanine thus are obtained directly in a single operation.Subjecting the monoalkylated material, N-(ethylamino)diacetic acid di-tert-butyl ester 3b, to a second alkylation with dibenzyl bromoethylaminediacetate 5a affords mixed pentaester 2c in which the terminal carboxyl groups are differentiated as benzyl esters at one end and tert-butyl at the other.Both complete and selective deprotections of the differentiated carboxyl groups in pentaesters 2a, 2b, and 2c are possible, allowing specific control of the carboxyl functionality at each terminus.The enantiomeric composition of monoalkyl amino acids 3a and 3b was evaluated by derivatizing with (+)-α-methylbenzyl isocyanate to afford the corresponding ureas.Analysis of the ureas by HPLC established the enantiomeric purity in each case as > 99 percent, thereby also establishing the enantiomeric purity of dialkyl compounds as > 99percent.Pentaacid 2d readily forms an optically active metal chelate with yttrium(III) as a single diastereomer.
