Synthesis of N-Acylamino-Acid Derivatives of Cytisine
N-acylamino-acid derivatives of cytisine were prepared by reacting cytisine with methyl esters of aminoacid isocyanates.
Yazlovitskii,Garazd,Kartsev
p. 272 - 275
(2016/07/06)
Design, synthesis and biological evaluation of novel amino acid ureido derivatives as aminopeptidase N/CD13 inhibitors
A series of amino acid ureido derivatives as aminopeptidase N (APN/CD13) inhibitors were synthesized and evaluated for their APN inhibitory activities and anti-cancer effects. The results showed that most of these amino acid ureido derivatives exhibited good inhibition against APN, several of which were better than Bestatin. The most active compound 12j (IC50 = 1.1 μM, compared with Bestatin IC50 = 8.1 μM) not only possessed much better APN inhibitory activity and anti-proliferation effect on cancer cells, but also exhibited significant block effect of human cancer cell invasion compared with the positive control, Bestatin. These amino acid ureido derivatives could be possibly developed as new APN inhibitors for cancer chemotherapy in the future.
Su, Li,Jia, Yuping,Zhang, Lei,Xu, Yingying,Fang, Hao,Xu, Wenfang
experimental part
p. 3807 - 3815
(2012/08/27)
Isocyanates, Part 4.10 Convenient Phosgene-Free Method for the Synthesis and Derivatization of Enantiopure α-Isocyanato Carboxylic Acid Esters
A novel phosgene-free procedure for the synthesis of α-isocyanato carboxylic acid esters starting from α-amino acid esters has been achieved. The isocyanates are obtained enantiomerically pure (> 99% ee) by a DMAP-catalyzed isocyanation with di-tert-butyl
Kn?lker, Hans-Joachim,Braxmeier, Tobias
p. 925 - 928
(2007/10/03)
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