16002-29-2Relevant articles and documents
Enzymatic Hydrolyses of the ?-Symmetric Dicarboxylic Diesters Bearing a Sulfinyl Group as the Prochiral Center
Tamai, Satoshi,Miyauchi, Satoru,Morizane, Chikako,Miyagi, Kaname,Shimizu, Hisashi,et al.
, p. 2381 - 2384 (1994)
Enzymatic hydrolyses of the ?-symmetric dicarboxylic diesters bearing a sulfinyl group as the prochiral center were examined by employing porcine liver esterase and porcine pancreatic lipase.Eventually, their chiral half esters were elaborately obtained as the corresponding chiral phenacyl esters.The stereochemistry of the chiral half esters was determined by the X-ray analysis and their chemical correlations.
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Hiskey,R.G.,Harpp,D.N.
, p. 2014 - 2018 (1964)
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Scaffold Diversity Inspired by the Natural Product Evodiamine: Discovery of Highly Potent and Multitargeting Antitumor Agents
Wang, Shengzheng,Fang, Kun,Dong, Guoqiang,Chen, Shuqiang,Liu, Na,Miao, Zhenyuan,Yao, Jianzhong,Li, Jian,Zhang, Wannian,Sheng, Chunquan
, p. 6678 - 6696 (2015/09/07)
A critical question in natural product-based drug discovery is how to translate the product into drug-like molecules with optimal pharmacological properties. The generation of natural product-inspired scaffold diversity is an effective but challenging strategy to investigate the broader chemical space and identify promising drug leads. Extending our efforts to the natural product evodiamine, a diverse library containing 11 evodiamine-inspired novel scaffolds and their derivatives were designed and synthesized. Most of them showed good to excellent antitumor activity against various human cancer cell lines. In particular, 3-chloro-10-hydroxyl thio-evodiamine (66c) showed excellent in vitro and in vivo antitumor efficacy with good tolerability and low toxicity. Antitumor mechanism and target profiling studies indicate that compound 66c is the first-in-class triple topoisomerase I/topoisomerase II/tubulin inhibitor. Overall, this study provided an effective strategy for natural product-based drug discovery. (Figure Presented).
PROCESS FOR PREPARING DIALKYL THIODIGLYCOLATES
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Page/Page column 2, (2009/07/10)
A process is described for preparing alkyl thiodiglycolates of the general formula (I) [in-line-formulae]R—OOC—CH2-S—CH2-COO—R ??(I)[/in-line-formulae] where R is a radical of branched or unbranched C1 to C10-alkyl, characterized in that an alkyl haloacetate of the general formula (II) [in-line-formulae]X—CH2-COO—R ??(II)[/in-line-formulae] where X is a chlorine or bromine atom and R is as defined for compounds of the formula (I) is reacted with an aqueous solution of alkali metal sulphide or alkali metal hydrogensulphide in the presence of an aqueous pH buffer solution in the pH range between 5 and 8, optionally in the presence of a phase transfer catalyst.