13030-09-6Relevant articles and documents
High selective autocatalytic esterification of glutamic acid by benzyl alcohol with CuCl2 promoting
Ma, Yinggai,Li, Zhenhuan,Su, Kunmei,Cheng, Bowen
, p. 15 - 18 (2014)
We found that the esterification of l-glutamic acid by benzyl alcohol is greatly promoted by CuCl2 even in H2O solvent, and the selectivity and yield of γ-benzyl ester of l-glutamic acid achieved 100% and 95.31%. Metal cation coordin
Synthesis and cytotoxic activities of β-carboline amino acid ester conjugates
Zhao, Ming,Bi, Lanrong,Wang, Wei,Wang, Chao,Baudy-Floc'h, Michele,Ju, Jingfang,Peng, Shiqi
, p. 6998 - 7010 (2006)
β-Carboline represents a class of compounds with potent anti-tumor activity by intercalating with DNA. To further enhance the cytotoxic potency and bioavailability of β-carboline, a series of novel β-carboline amino acid ester conjugates were designed and synthesized, and the cytotoxic activities of these compounds were tested using a panel of human tumor cell lines. In addition, the membrane permeability of these compounds was evaluated in vitro using a Caco-2 cell monolayer model. The β-carboline amino acid ester conjugates demonstrated improved cytotoxic activity compared to the parental β-carbolines. In particular, the Lys/Arg conjugates were the most potent analogs with an IC50 value of 4 and 1 μM against human cervical carcinoma cells. The low interaction energy of Arg conjugate based on molecular modeling may contribute to its enhanced cytotoxicity. Taken together, this study provided new insights into structure-activity relationships in the β-carboline amino acid ester conjugates and identified the β-carboline Lys/Arg conjugates as promising lead compounds for further in vivo biological and molecular evaluation.
SMALL MOLECULE VE-PTP INHIBITORS
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Page/Page column 117, (2022/01/05)
The present disclosure relates to compounds capable of inhibiting vascular endothelial protein tyrosine phosphatase (VE-PTP). These compounds are also capable of activating Tie2 receptor-mediated signaling. The present disclosure also relates to pharmaceutically acceptable salts of said compounds, to pharmaceutical compositions comprising such compounds and/or pharmaceutically acceptable salts thereof, and to the use of such compounds, pharmaceutically acceptable salts thereof, and/or pharmaceutical compositions comprising the same in treating diseases and/or conditions mediated by VE-PTP signaling, such as those mediated by Angiopoietm/Tie2 signaling.
Peptide Synthesis in Aqueous Solution. V. Properties and Reactivities of (p-Hydroxyphenyl)benzylmethylsulfonium Salts for Direct Benzyl Esterification of N-Acylpeptides
Nakata, Takashi,Nakatani, Masaru,Takahashi, Masatoshi,Okai, Jiro,Kawaoka, Yoshiaki,Kouge, Katsushige,Okai, Hideo
, p. 1099 - 1106 (2007/10/03)
Some (p-hydroxyphenyl)benzylmethylsulfonium salts were prepared. These compounds generated a benzyl cation and converted not only N-acylamino acids but also N-acylpeptides into their corresponding benzyl esters without causing the racemization.