6313-36-6Relevant articles and documents
Spectroscopic characterization of 1:1 complexes of some carbon acids activated by two sulfonyl groups with 1,5,7-triazabicyclo[4.4.0]dec-5-ene in acetonitrile
Binkowska, Iwona
, p. 56 - 65 (2014)
The series of six carbon acids activated by two sulfonyl groups have been synthesized and the products of their deprotonation in acetonitrile solution by 1,5,7-triazabicyclo[4.4.0]dec-5-ene (TBD) were defined by electrospray ionization mass spectrometry method. The deprotonation of carbon acids and derivative fragmentary carbanions at various cone voltage are compared. Substituent effect on the fragmentation of molecular anions and heats of formation are reported. The fragmentation pathways of the carbanions of studied carbon acids are proposed and the differences in fragmentation of these ions are discussed. The calculated heats of formation of molecular and fragmentary carbanions reveal good Hammett plots against σ values.
Narciclasine derivative, and preparation and application thereof in preparation of antitumor drugs
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Paragraph 0063; 0076; 0077; 0078, (2017/04/28)
The invention provides a narciclasine derivative represented by the following structural formula I, wherein R1 is alkyl, cycloalkyl, benzyl or substituted benzyl, R2 is alkyl, cycloalkyl, benzyl or substituted benzyl, and n is an integer from 1 to 10. The narciclasine derivative is subjected to a tumor cell toxicity killing effect test, and results prove that the narciclasine derivative has strong toxicity killing effects on lung gland tumor cells, intestinal tumor cells, breast tumor cells, liver tumor cells, prostate tumor cells, melanoma tumor cells, endometrial tumor cells and neuroglia tumor cells, so the narciclasine derivative can be used for preparation of antitumor drugs. The invention provides a preparation method of the narciclasine derivative. The narciclasine derivative has a novel side-chain structure, shows excellent inhibitory activity on a variety of tumor cell strains, has drug efficacy better than that of narciclasine, allows toxic and side effects of the compound to be improved, provides new drugs for treatment of malignant tumors, and is of great clinical application value.
Design, synthesis and biological evaluation of brain-targeted thiamine disulfide prodrugs of ampakine compound LCX001
Xiao, Dian,Meng, Fan-Hua,Dai, Wei,Yong, Zheng,Liu, Jin-Qiu,Zhou, Xin-Bo,Li, Song
, (2016/05/24)
: Ampakine compounds have been shown to reverse opiate-induced respiratory depression by activation of amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) glutamate receptors. However, their pharmacological exploitations are hindered by low blood-brain barrier (BBB) permeability and limited brain distribution. Here, we explored whether thiamine disulfide prodrugs with the ability of "lock-in" can be used to solve these problems. A series of thiamine disulfide prodrugs 7a-7f of ampakine compound LCX001 was synthesized and evaluated. The trials in vitro showed that prodrugs 7e, 7d, 7f possessed a certain stability in plasma and quickly decomposed in brain homogenate by the disulfide reductase. In vivo, prodrug 7e decreased the peripheral distribution of LCX001 and significantly increased brain distribution of LCX001 after i.v. administration. This compound showed 2.23- and 3.29-fold greater increases in the AUC0-t and MRT0-t of LCX001 in brain, respectively, than did LCX001 itself. A preliminary pharmacodynamic study indicated that the required molar dose of prodrug 7e was only one eighth that of LCX001 required to achieve the same effect in mice. These findings provide an important reference to evaluate the clinical outlook of ampakine compounds.
