- Hydrogen-bonding-induced bathochromic effect of Si-coumarin and its use in monitoring adipogenic differentiation
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Introduction of a heteroatom into a fluorophore was carried out for coumarin through a replacement of its bridging oxygen atom with a silicon atom. The maximum-emission wavelength of Si-coumarin (SiC B) bathochromically shifted from 426 nm in cyclohexane to 626 nm in water. The adipogenic differentiation processes in mesenchymal stem cells were monitored using SiC B.
- Li, Chen,Wang, Ting,Li, Ni,Li, Min,Li, Yuntao,Sun, Yan,Tian, Yang,Zhu, Junru,Wu, Yiqian,Zhang, Dazhi,Cui, Xiaoyan
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Read Online
- Design, synthesis, and biological evaluation of novel triazoloquinazolinone derivatives as SHP2 protein inhibitors
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A novel series of triazoloquinazolinone derivatives were designed, synthesised, and evaluated for their in vitro biological activities against the SHP2 protein. Moreover, some compounds were evaluated against A375 cells. The results revealed that target compounds possessed moderate to excellent inhibitory activity against SHP2 protein, whereas compounds 12f, 12l, 12j, 17e, and 17f have strong antiproliferative activity on A375 cells. The compound 12l showed remarkable cytotoxicity against A375 cells and a strong inhibitory effect against SHP2 protein when compared with SHP244. The structure-activity relationships (SARs) indicated that electron-donating groups (EDGs) on phenyl rings are beneficial for improving the antitumor activity; compounds with a hydroxyl substituent at the 2-position of phenyl ring exhibited superior activities than compounds with a substituent at the 4-position. In addition, compound 12l displayed improved physicochemical properties as well as metabolic stability compared to SHP244. Our efforts identified 12l as a promising SHP2 protein inhibitor, warranting its further investigation.
- Huang, Zhuyan,Lu, Tian,Luo, Dali,Luo, Rongshuang,Qin, Yumei,Wang, Zhongyuan,Yang, Di,Zhao, Chunshen,Zhou, Zhixu
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p. 2170 - 2182
(2021/11/17)
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- A class of silicon-substituted coumarin derivatives, and synthesis method thereof
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The invention discloses a class of silicon-substituted coumarin derivatives, which have a structure represented by a formula I, wherein R is a nitrogen methyl group, a nitrogen ethyl group, a nitrogenhydrogen ethyl group, a nitrogen four-membered ring, a nitrogen ethyl five-membered ring or a nitrogen ethyl six-membered ring. According to the preparation, aniline is subjected to a formylation reaction by using a corresponding aromatic amine as a starting raw material and using phosphorus oxychloride and DMF as reaction reagents; the Ylide reaction of the aldehyde group is performed by using n-butyl lithium as a reaction reagent and using anhydrous THF as a solvent; a lithiation reaction is performed by using n-butyl lithium as reaction reagent to obtain a dimethyl silicon substituted intermediate; and finally diene is subjected to a double decomposition reaction under the catalysis of a Grubbs II catalyst to achieve the intramolecular ring closure, and oxidation is performed with selenium dioxide to obtain the final product. According to the present invention, a class of the novel silicon-substituted coumarin derivatives are synthesized, are sensitive to environmental polarity, and can be used for monitoring the activity of cells in vivo.
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Paragraph 0046-0051; 0053
(2019/10/01)
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- Synthesis of unsymmetrical Si-rhodamine fluorophores and application to a far-red to near-infrared fluorescence probe for hypoxia
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Si-Rhodamines are bright fluorophores with red to near-infrared (NIR) emission, and are widely used for fluorescence imaging of biological phenomena. Here, in order to extend the scope of Si-rhodamine fluorophores, we established a versatile synthesis of unsymmetrical Si-rhodamines. To illustrate its value, we used one of these new fluorophores to synthesize a far-red to NIR fluorescence probe for hypoxia, and showed that it can visualize hepatic ischemia in mice in vivo.
- Hanaoka, Kenjiro,Kagami, Yu,Piao, Wen,Myochin, Takuya,Numasawa, Koji,Kuriki, Yugo,Ikeno, Takayuki,Ueno, Tasuku,Komatsu, Toru,Terai, Takuya,Nagano, Tetsuo,Urano, Yasuteru
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supporting information
p. 6939 - 6942
(2018/06/26)
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- NEAR-INFRARED FLUORESCENT DYES AND USES THEREOF
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The invention relates to a near-infrared fluorescent dye and use thereof, and particularly relates to compounds represented by following Formulae A, B and C, wherein each group in the Formulae is described in the specification. Further provided are a dye
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Paragraph 0079
(2018/10/30)
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- Micromolecular fluorescent probe capable of quantitatively detecting Hg and MeHg
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The invention provides a micromolecular fluorescent probe capable of quantitatively detecting Hg and MeHg, a detection composition and detection kit containing the micromolecular fluorescent probe and a method for detecting the Hg and/or the Me
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Paragraph 0077; 0079
(2017/02/09)
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- Synthesis of Sterically Protected Xanthene Dyes with Bulky Groups at C-3′ and C-7′
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Substitution of the xanthene scaffold with bulky groups at C-3′ and C-7′ is expected to protect the electrophilic central methine carbon against nucleophilic attack and inhibit stacking. However, such structures are not readily prepared via traditional xa
- Lei, Zuhai,Li, Xinran,Li, Yi,Luo, Xiao,Zhou, Miaomiao,Yang, Youjun
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p. 11538 - 11543
(2015/12/01)
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