31302-84-8Relevant articles and documents
Lipase from Carica papaya latex presents high enantioselectivity toward the resolution of prodrug (R,S)-2-bromophenylacetic acid octyl ester
Rivera, Ivanna,Mateos, Juan Carlos,Marty, Alain,Sandoval, Georgina,Duquesne, Sophie
, p. 5523 - 5526 (2013)
Besides the well-known papain, lipolytic activity is another interesting enzymatic activity present in latex from Carica papaya. This lipolytic activity is strongly attached to the latex solid phase, resulting in a naturally immobilized biocatalyst. In this work we describe the kinetic resolution of (R,S)-2-bromophenylacetic acid octyl ester by Carica papaya crude latex and two partially purified latex fractions. Several parameters, such as substrate concentration and solvent effects were studied. The best results were obtained using decane as solvent with 50 mM of substrate and 50 mg/mL enzyme/reaction medium; under these conditions, a high enantioselectivity (E >200) was obtained with crude latex. A twofold increase of the initial rate maintaining E >200 was obtained using purified fractions without protease and without esterase. Lipase from Carica papaya latex is the most enantioselective wild-type enzyme ever described for the studied reaction.
Novel synthetic method of D/L-phenyl glycine
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Paragraph 0022-0025, (2020/04/22)
The invention relates to a novel synthetic method of D/L-phenyl glycine. An existing synthetic method of D/L-phenylglycine is used for producing D/L-phenyl glycine by using highly toxic raw materials,and the synthetic method is harmful. According to the synthesis method, benzene is used as a solvent and a raw material. The method comprises the following steps: firstly, performing Friedel-Crafts alkylation reaction between benzene and dichloroacetic acid or bromochloroacetic acid under the catalystic function of a catalyst, wherein the reaction temperature of Friedel-Crafts alkylation reactionis 55-60 DEG C, the reaction time is 7h, and after Friedel-Crafts alkylation reaction, a benzene solution of alpha-chlorophenylacetic acid or alpha-bromophenylacetic acid is obtained; separating thereaction product into a water phase by using 20% ammonia water; adding urotropin into the water phase to carry out catalytic reactions at a temperature of 75-80 DEG C for 12 hours, controlling the temperature to be 70-80 DEG C, neutralizing the solution by 30% sulfuric acid until the pH value is equal to 6.5 to obtain a D/L-phenyl glycine water solution, and performing suction filtration to obtaina filter cake, namely D/L-phenyl glycine. Cyanide is not used, production is safe, energy consumption is reduced, and the raw material quality standard of downstream products is met.
Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer
Xue, Xiaoqian,Zhang, Yan,Wang, Chao,Zhang, Maofeng,Xiang, Qiuping,Wang, Junjian,Wang, Anhui,Li, Chenchang,Zhang, Cheng,Zou, Lingjiao,Wang, Rui,Wu, Shuang,Lu, Yongzhi,Chen, Hongwu,Ding, Ke,Li, Guohui,Xu, Yong
supporting information, p. 542 - 559 (2018/05/24)
The bromodomain and extra-terminal proteins (BET) have emerged as promising therapeutic targets for the treatment of castration-resistant prostate cancer (CRPC). We report the design, synthesis and evaluation of a new series of benzoxazinone-containing 3,5-dimethylisoxazole derivatives as selective BET inhibitors. One of the new compounds, (R)-12 (Y02234), binds to BRD4(1) with a Kd value of 110 nM and blocks bromodomain and acetyl lysine interactions with an IC50 value of 100 nM. It also exhibits selectivity for BET over non-BET bromodomain proteins and demonstrates reasonable anti-proliferation and colony formation inhibition effect in prostate cancer cell lines such as 22Rv1 and C4-2B. The BRD4 inhibitor (R)-12 also significantly suppresses the expression of ERG, Myc and AR target gene PSA at the mRNA level in prostate cancer cells. Treatment with (R)-12 significantly suppresses the tumor growth of prostate cancer (TGI = 70%) in a 22Rv1-derived xenograft model. These data suggest that compound (R)-12 is a promising lead compound for the development of a new class of therapeutics for the treatment of CRPC.
