2199-59-9Relevant articles and documents
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Corwin,Andrews
, p. 1086,1088 (1936)
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Conformationally Induced Off-On Cell Membrane Chemosensor Targeting Receptor Protein-Tyrosine Kinases for in Vivo and in Vitro Fluorescence Imaging of Cancers
Jiao, Yang,Yin, Jiqiu,He, Haiyang,Peng, Xiaojun,Gao, Qianmiao,Duan, Chunying
, p. 5882 - 5885 (2018)
Molecules capable of monitoring receptor protein-tyrosine kinase expression could potentially serve as useful tools for cancer diagnosis due to the overexpression of tyrosine kinases during tumor growth and metastasis. In this work, a conformationally induced "off-on" tyrosine kinase cell membrane fluorescent sensor (SP1) was designed and evaluated for the detection and imaging of receptor protein-tyrosine kinases in vivo and in vitro. SP1 consists of sunitinib and pyrene linked via hexamethylenediamine and displays quenched fluorescence as a dimer. The fluorescence of SP1 is restored in the presence of receptor protein-tyrosine kinases upon strong interaction with SP1 at the target terminal. The unique signal response mechanism enables SP1 use for fluorescence microscopy imaging of receptor protein-tyrosine kinases in the cell membranes of living cells, allowing for the rapid differentiation of cancer cells from normal cells. SP1 can be used to visualize the chick embryo chorioallantoic membrane and mouse model tumors, suggesting its possible application for early cancer diagnosis.
Antimicrobial and antiproliferative study of chalcone clubbed 2,4-dimethylpyrrole-3-carboxamide derivatives: Synthesis and in vitro evaluation
Rasal, Nishant Kisan,Jagtap, Sangeeta Vijay,Bhange, Dattatraya Soma
, p. 119 - 130 (2021/10/06)
The presented study explores the anticancer potency of a novel series of chalcone clubbed 2,4-dimethyl-1H-pyrrole-3-carboxamide derivatives. In vitro antimicrobial screening concluded that five compounds are potential against Candida albicans having inhibition of growth in the range of 46.38%–73.05% against at the concentration of 32 μg/mL. The antiproliferative screening against 60 cancer cell lines revealed that seven compounds have great potential against the various types of cancer cell lines with inhibition of growth in the range of 41%–71%. The structure–activity relationship study concluded that the hydrazide bond is more significant than the carboxamide bond. In silico study of highly potential derivatives obeys each parameter of Lipinski rule of five and qualified drug-likeness behavior. The presented pyrrole-chalcone template delivered various candidates as anticancer agents, and those could be a potential scaffold to develop the new anticancer drug.
IBX-TfOH mediated oxidation of alcohols to aldehydes and ketones under mild reaction conditions
Kumar, Kamlesh,Kumar, Prashant,Joshi, Penny,Rawat, Diwan S
supporting information, (2020/03/04)
An efficient, practical and facile procedure has been developed for the oxidation of primary and secondary alcohols using IBX-TfOH catalytic system in 1,4-dioxane at ambient temperature. The reaction affords quantitative yields of the corresponding carbonyl compounds without the formation of over oxidized products. The present synthetic protocol is compatible with a variety of substrates having arene, heteroarene and alkene functionalities. The developed synthetic protocol can be used for higher scale reactions as evident by the oxidation of alcohol at 1 g scale in higher yields by a simple filtration process.
Enhanced fluorescence sensor for targeting recognition of receptor tyrosine kinase and application of fluorescence sensor in cell membrane fluorescence imaging
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Paragraph 0014; 0015, (2019/02/13)
The invention discloses an enhanced fluorescence sensor for targeting recognition of receptor tyrosine kinase and application of the fluorescence sensor in cell membrane fluorescence imaging, and belongs to the technical field of bioluminescence sensing. Effective parts of sunitinib are adopted as recognition groups of the fluorescence sensor SP1, pyrene is adopted as a fluorescent group, and connection is formed through linking groups; and the receptor tyrosine kinase which is protein on cell membranes is abundantly enriched in the process of generation of tumor cells and vessels. The fluorescent sensor SP1 can effectively act on the intracellular domains of the cell membranes of the receptor tyrosine kinase, and compared with amino acids, inorganic salts and other interfering substancesin cells, the fluorescence sensor SP1 exhibits high selectivity and a targeted recognition effect on the receptor tyrosine kinase; the SP1 has good selectivity and high sensitivity in recognition of the receptor tyrosine kinases, fluorescence imaging of the receptor tyrosine kinase can be achieved in the cells, tissue and living bodies, and the enhanced fluorescence sensor has potential application prospects in early cancer diagnosis, visualization therapy and other fields.