23451-95-8Relevant academic research and scientific papers
Synthesis and evaluation of novel benzothiazole derivatives based on the bithiophene structure as potential radiotracers for β-amyloid plaques in Alzheimer's disease
Cui, Meng-Chao,Li, Zi-Jing,Tang, Rui-Kun,Liu, Bo-Li
, p. 2777 - 2784 (2010)
In this study, six novel benzothiazole derivatives based on the bithiophene structure were developed as potential β-amyloid probes. In vitro binding studies using Aβ aggregates showed that all of them demonstrated high binding affinities with Ki/sub
Facile syntheses of 3-trifluoromethylthio substituted thioflavones and benzothiophenes via the radical cyclization
Wang, Lu,Wang, Huaiyu,Meng, Weidong,Xu, Xiu-Hua,Huang, Yangen
supporting information, p. 389 - 392 (2020/03/04)
3-CF3S substituted thioflavones and benzothiophenes were achieved via the reactions of AgSCF3 with methylthiolated alkynones and alkynylthioanisoles, respectively, promoted by persulfate. This protocol possesses good functional group tolerance and high yields. Mechanistic studies suggested that a classic two-step radical process was involved, which includes addition of CF3S radical to triple bond and cyclization with SMe moiety.
Design, synthesis and biological evaluation of benz-fused five-membered heterocyclic compounds as tubulin polymerization inhibitors with anticancer activities
Komuraiah, Buduma,Ren, Yichang,Xue, Mingming,Cheng, Binbin,Liu, Jin,Liu, Yao,Chen, Jianjun
, p. 1109 - 1116 (2021/03/16)
A series of benz-fused five-membered heterocyclic compounds were designed and synthesized as novel tubulin inhibitors targeting the colchicine binding site. Among them, compound 4d displayed the highest antiproliferative activity against four cancer cell lines with an IC50 value of 4.9?μM in B16-F10 cells. Compound 4d effectively inhibited tubulin polymerization in vitro (IC50 of 13.1?μM). Further, 4d induced cell cycle arrest in G2/M phase. Finally, 4d inhibited the migration of cancer cells in a dose-dependent manner. In summary, these results suggest that compound 4d represents a new class of tubulin inhibitors deserving further investigation.
Convenient and efficient synthesis of novel 11: H -benzo[5,6][1,4]thiazino[3,4- a] isoindol-11-ones derived from 2-bromo-(2/3-substitutedphenyl)-1 H -indene-1,3(2 H)-diones
Mor, Satbir,Sindhu, Suchita
, p. 12784 - 12792 (2019/05/10)
An unprecedented formation of 11H-benzo[5,6][1,4]thiazino[3,4-a]isoindol-11-ones through a one-step reaction of differently substituted 2-aminobenzenethiols and 2-bromo-(2/3-substitutedphenyl)-1H-indene-1,3(2H)-diones in freshly dried ethanol under reflux conditions has been investigated. This unique transformation probably occurs through an initial nucleophilic substitution followed by ring opening and subsequent intramolecular cyclization. The structures of all the synthesized benzo[1,4]thiazino isoindolinones were established by FTIR, 1H NMR, 13C NMR, HRMS, and X-ray crystallographic analysis. This approach was found to be simple and convenient and provides several advantages such as substantial atom economy, short reaction time and operational simplicity.
For the preparation and β Amyloid protein specific binding of the compound of compound, preparation method and application thereof (by machine translation)
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Paragraph 0050; 0065; 0072, (2018/07/30)
One aspect of the invention discloses a compound, the compound has the structural formula X as shown in the structure, wherein the substituted group R1 Can be - NO2 It also can be thought that the - NHCH3 ; On the other ha
Compound for preparing compound specifically bound with beta amyloid protein, preparation method and application thereof
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Paragraph 0057; 0064, (2018/07/30)
The invention discloses a compound on one hand, wherein the compound has a structure as shown in structural formula A as shown in the specification, and a substituent group R1 can be -NO2, and also can be -NH2; and the invention discloses application of t
COMPOUND FOR SPECIFICALLY BINDING TO AMYLOID ?-PROTEIN
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Paragraph 0062-0065, (2018/11/21)
Provided is a compound for specifically binding to amyloid β-protein. The compound has thereon a nuclide with a large thermal neutron capture cross section and the compound is capable of specifically binding to the amyloid β-protein. The property of the compound allows it to be used in conjunction with a neutron capture therapy device to eliminate amyloid β-protein. Similarly, when the compound is labelled with radioactive element 11C, the compound can also be used in conjunction with PET/CT for determining the part of the brain where amyloid β-protein is deposited, for diagnosing Alzheimer's disease. Also disclosed is a preparation process for the compound. The beneficial effect of the present disclosure is to make the therapy and diagnosis of Alzheimer's disease more targeted by providing the compound for specifically binding to amyloid β-protein.
Erratum: Genetically encoded multispectral labeling of proteins with polyfluorophores on a DNA backbone (Journal of the American Chemical Society (2013) 135 (6184-6191) DOI: 10.1021/ja4004393)
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supporting information, p. 2118 - 2118 (2017/02/15)
A n internal review of our NMR data in the published Supporting Information (SI) file revealed that one of the authors (V.S.) had digitally removed peaks of impurities and solvents from some of the spectra. To correct this, we now provide a new version of the SI file with the unaltered spectra. Two new authors (K.M.C., S.A.C.) have recharacterized the original haloalkyl reagent B8 and have confirmed its identity by NMR and mass spectrometry. In addition, we have confirmed the identity of one of the original dyes by MALDI-TOF mass spectrometry, and used it successfully to label bacteria expressing a HaloTag fusion; these data are added to the corrected SI file. We stand by the conclusions of the article, and we regret the publication of the altered characterization data. We also correct the author list to include the scientists (K.M.C. and S.A.C.) who worked to independently check the data and conclusions. The new author list should read as follows: Vijay Singh, Shenliang Wang, Ke Min Chan, Spencer A. Clark, and Eric T. Kool.
Synthesis of Indane-Based 1,5-Benzothiazepines Derived from 3-Phenyl-2,3-dihydro-1H-inden-1-one and Antimicrobial Studies Thereof
Mor, Satbir,Nagoria, Savita,Sindhu, Suchita,Khatri, Mohini,Sidhu, Gurdeep,Singh, Virender
, p. 3282 - 3293 (2017/10/06)
In the present study, a series of 20 indane-based 1,5-benzothiazepines (5a–t) has been prepared derived from 3-phenyl-2,3-dihydro-1H-inden-1-one (1). All the synthesized 1,5-benzothiazepines (5a–t) were screened for their in vitro antimicrobial activities against four bacteria [Bacillus subtilis (MTCC 441), Staphylococcus epidermidis (MTCC 6880), Escherichia coli (MTCC 1652), and Pseudomonas aeruginosa (MTCC 424)] and two fungi [Candida albicans (MTCC 227) and Aspergillus niger (MTCC 8189)]. Among all the tested derivatives, 5n and 5o against E.?coli displayed more inhibitory activity than that of the reference drug, ciprofloxacin, while the derivatives 5c, 5m–o, 5s, and 5t against C.?albicans, and 5d, 5e, 5n, 5o, 5s, and 5t against A.?niger were found to be more potent than the standard drug, that is, fluconazole.
Neutron capture therapy system for removing amyloid beta-protein employing neutron beam source to destroy structure of amyloid beta-protein for removal without damaging normal tissues
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Paragraph 0071; 0077; 0093, (2018/02/13)
The present invention provides a neutron capture therapy system for removing amyloid beta-protein, which comprises a neutron capture therapy device and a compound containing nuclides with large thermal neutron capture crossed section capable of heterogene
