104060-53-9Relevant academic research and scientific papers
Development of synthetic aminopeptidase N/CD13 inhibitors to overcome cancer metastasis and angiogenesis
Su, Li,Cao, Jiangying,Jia, Yuping,Zhang, Xiaonan,Fang, Hao,Xu, Wenfang
, p. 959 - 964 (2013/02/23)
Cancer metastasis is a major barrier to its treatment and an important cause of patient death. Antimetastatic agents hold promise for patients with advanced metastatic tumors. Aminopeptidase N/CD13 (APN) is being pursued by many as an important target against cancer metastasis and angiogenesis, but there are few reports on the in vivo evaluation of synthetic APN inhibitors. Herein, a series of compounds targeting APN were synthesized and evaluated for their antimetastasis and antiangiogenesis potency both in vitro and in vivo. Excitingly, compounds 4m, 4t, and 4cc, with the most potent APN inhibitory activities, displayed significant antimetastasis and antiangiogenesis effects in vitro and in vivo, suggesting that those synthetic APN inhibitors have the potential to overcome cancer metastasis and angiogenesis.
Synthesis of novel chiral cholic acid-based molecular tweezers containing unsymmetrically disubstituted urea units using microwave irradiation
Zeng, Bitao,Zhao, Zhigang,Zhou, Lijun,Li, Qinghan
scheme or table, p. 206 - 209 (2012/09/08)
An efficient procedure has been developed for the synthesis of new chiral cholic acid molecular tweezer artificial receptors by linking an unsymmetrically disubstituted urea to methyl deoxycholate via a carbonate chain using microwave irradiation. The structures of these new receptors were confirmed by 1H NMR, IR, MS spectra and elemental analysis. Their binding properties were examined by UV-Vis spectra titration. The preliminary results indicate that these molecular tweezers not only recognised anions, but also showed good enantioselectivity for D-amino acid methyl esters.
Solvent-free synthesis of novel chiral unsymmetrical urea molecular tweezers under microwave irradiation
Zhao, Zhigang,Xia, Zhenyang,Li, Xiaorui,Shi, Peiyu
scheme or table, p. 47 - 50 (2011/05/04)
Seven novel chiral unsymmetrical urea molecular tweezers based on 1, 3-phenoxyacetic acid have been designed and synthesised using solid K 2CO3 as supporter in the solvent-free conditions under microwave irradiation. This method is simple, fast, efficient and eco-friendly. The structures of target compounds were characterised by IR, 1H NMR, MS spectra and elemental analyses and their molecular recognition properties were investigated by UV-Vis spectral titration. The preliminary results indicated that these molecular tweezers possess good selectivity for D/L amino acid methyl esters and some anions.
The synthesis of novel chiral cholic acid-based molecular clefts containing unsymmetrically disubstituted urea unit
Mu, Qi Ming,Xue, Cui Hua,Zhang, Qing Hua,Chen, Shu Hua
, p. 3055 - 3061 (2007/10/03)
A novel type of chiral molecular clefts has been designed and synthesized by linking an unsymmetrically disubstituted urea to methyl deoxycholate via a carbonate chain. The structures of these new receptors 3a-d were confirmed by 1H NMR, IR, MS
Solid-phase synthesis of oligourea peptidomimetics
Boeijen, Astrid,Liskamp, Rob M. J.
, p. 2127 - 2135 (2007/10/03)
A procedure for the solid-phase synthesis of oligourea peptidomimetics starting from Boc-protected monomers is described. The compounds are prepared on Tentagel resin and can be obtained selectively rather as the C-terminal free acids with UV irradiation
Chiral Analysis of Synthetic Peptides: High Performance Liquid Chromatography of Diastereoisomeric Carbamoyl Esters derived from N-Terminal Cleavage
Davies, John S.,Enjalbal, Christine,Llewellyn, Gareth
, p. 1225 - 1231 (2007/10/02)
A cleavage routine for chiral analysis has revealed that the N-terminal residue in model dipeptides, after derivatisation with a chiral isocyanate reagent, can be cleaved off as the N-carbamoyl ester under relatively mild conditions (MeOH/SOCl2/60 deg C f
