25458-44-0Relevant articles and documents
First total synthesis of mariamide A
Xia, Yamu,Chen, Chenglong,Li, Mengying,Zhou, Weizeng,Sun, Shuyu,Chu, Shanpeng,Wang, Hui
, p. 114 - 120 (2020)
Mariamide A, a lignanamide isolated from the seeds of Silybum marianum, has demonstrated potential utility as an antioxidant and antidiabetic agent and possesses an 8-O-4′ neolignan skeleton. Herein, a first total synthesis of mariamide A is presented that proceeds in nine steps using vanillin as the starting material. The key steps for the preparation of mariamide A involve an I2-catalyzed bromomethoxylation of an alkene group, a nucleophilic substitution followed by a sequential elimination and a monoacylation reaction.
Carbosilane Glycodendrimers for Anticancer Drug Delivery: Synthetic Route, Characterization, and Biological Effect of Glycodendrimer-Doxorubicin Complexes
Müllerová, Monika,Maciel, Dina,Nunes, Nádia,Wrobel, Dominika,Stofik, Marcel,?ervenková ?tastná, Lucie,Krupková, Alena,Cu?ínová, Petra,Nováková, Kate?ina,Bo?ík, Matěj,Maly, Marek,Maly, Jan,Rodrigues, Jo?o,Stra?ák, Tomá?
, p. 276 - 290 (2022/01/04)
The complexity of drug delivery mechanisms calls for the development of new transport system designs. Here, we report a robust synthetic procedure toward stable glycodendrimer (glyco-DDM) series bearing glucose, galactose, and oligo(ethylene glycol)-modified galactose peripheral units. In vitro cytotoxicity assays showed exceptional biocompatibility of the glyco-DDMs. To demonstrate applicability in drug delivery, the anticancer agent doxorubicin (DOX) was encapsulated in the glyco-DDM structure. The anticancer activity of the resulting glyco-DDM/DOX complexes was evaluated on the noncancerous (BJ) and cancerous (MCF-7 and A2780) cell lines, revealing their promising generation- and concentration-dependent effect. The glyco-DDM/DOX complexes show gradual and pH-dependent DOX release profiles. Fluorescence spectra elucidated the encapsulation process. Confocal fluorescence microscopy demonstrated preferential cancer cell internalization of the glyco-DDM/DOX complexes. The conclusions were supported by computer modeling. Overall, our results are consistent with the assumption that novel glyco-DDMs and their drug complexes are very promising in drug delivery and related applications.
S1P1 AGONIST AND APPLICATION THEREOF
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Paragraph 0345; 0349-0351, (2021/10/02)
The present invention relates to a class of tricyclic compounds and an application thereof as a sphingosine 1-phosphate type 1 (S1P1) receptor agonist. The invention specifically relates to a compound represented by formula (II), and a tautomer and pharmaceutically acceptable salt of same.
Discovery of deoxyceramide analogs as highly selective ACER3 inhibitors in live cells
Bielsa, Núria,Casasampere, Mireia,Aseeri, Mazen,Casas, Josefina,Delgado, Antonio,Abad, José Luis,Fabriàs, Gemma
, (2021/03/08)
Acid (AC), neutral (NC) and alkaline ceramidase 3 (ACER3) are the most ubiquitous ceramidases and their therapeutic interest as targets in cancer diseases has been well sustained. This supports the importance of discovering potent and specific inhibitors
COMPOSITIONS AND METHODS OF MODULATING SHORT-CHAIN DEHYDROGENASE ACTIVITY
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, (2020/06/10)
Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors described herein.
Synthesis of (3-(2-aminopyrimidin-4-yl)-4-hydroxyphenyl)phenyl methanone analogues as inhibitors of vascular endothelial growth factor receptor-2 kinase
More, Kunal N.,Lee, Jinho
, p. 70 - 77 (2017/01/16)
Angiogenesis is critical for tumor growth and mediated mainly by vascular endothelial growth factor (VEGF) signaling. Inhibition of the VEGF signaling pathway has emerged as one of the promising approaches for cancer therapy. VEGF receptor 2 (VEGFR-2) is
First total synthesis of quiquesetinerviusin A
Xia, Yamu,Mo, Zhen,Sun, Lin,Zou, Lijia,Zhang, Wen,Zhang, Jiahong,Wang, Lihong
, p. 296 - 300 (2017/06/19)
The first total synthesis of the dihydrobenzofuran neolignan quiquesetinerviusin A and its related structure have been described. Phenolic coupling is the key step to constructing the dihydrobenzofuran skeleton with vanillin as the raw material. The hydroxyl group was protected with dihydropyran (DHP) and the ester group was reduced with diisobutylaluminium hydride (DIBAL-H) in order to obtain the crucial intermediate diol, which was then condensed with an acid ligand to give the desired compounds following removal of the protecting groups.
Rhodium-Catalyzed Decarbonylative Borylation of Aromatic Thioesters for Facile Diversification of Aromatic Carboxylic Acids
Ochiai, Hidenori,Uetake, Yuta,Niwa, Takashi,Hosoya, Takamitsu
supporting information, p. 2482 - 2486 (2017/02/23)
Transformation of aromatic thioesters into arylboronic esters was achieved efficiently using a rhodium catalyst. The broad functional-group tolerance and mild conditions of the method have allowed for the two-step decarboxylative borylation of a wide range of aromatic carboxylic acids, including commercially available drugs.
Compound has the negative light dispersion, negative dispersion of this compound-containing composition and containing the composition for preparing anisotropic optical (by machine translation)
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Paragraph 0352; 0353, (2016/10/09)
The invention relates to a kind of reverse wdxrf compound, containing the compound reverse of wavelength dispersion composition and containing the optical anisotropic body. According to the present invention the reverse of wavelength dispersion composition is capable of providing a stronger and more stable reverse wdxrf nature, and can offer excellent optical performance of the optical anisotropic body. (by machine translation)
COMPOUNDS HAVING NEGATIVE OPTICAL DISPERSION, NEGATIVE OPTICAL DISPERSION COMPOSITION COMPRISING THE COMPOUNDS, AND OPTICALLY ANISOTROPIC BODY COMPRISING THE COMPOSITION (As Amended)
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Paragraph 0232, (2016/08/17)
The present invention relates to a reverse wavelength dispersion compound, a reverse wavelength dispersion composition including the same, and an optically anisotropic body including the same. The reverse wavelength dispersion composition according to the present invention can provide a stronger and more stable reverse wavelength dispersion property, and makes it possible to provide an optically anisotropic body having excellent optical properties.
