14482-32-7Relevant academic research and scientific papers
Functionalized tricyclic cytosine analogues provide nucleoside fluorophores with improved photophysical properties and a range of solvent sensitivities
Rodgers, Brittney J.,Elsharif, Nada A.,Vashisht, Nisha,Mingus, MacY M.,Mulvahill, Mark A.,Stengel, Gudrun,Kuchta, Robert D.,Purse, Byron W.
, p. 2010 - 2015 (2014)
Tricyclic cytosines (tC and tCO frameworks) have emerged as a unique class of fluorescent nucleobase analogues that minimally perturb the structure of B-form DNA and that are not quenched in duplex nucleic acids. Systematic derivatization of th
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.
CURABLE COMPOSITION, CURED FILM, OPTICAL FILTER, SOLID IMAGE PICKUP ELEMENT, IMAGE DISPLAY DEVICE, INFRARED SENSOR, DISPERSING AUXILIARY AGENT, DISPERSION, AND METHOD OF MANUFACTURING DISPERSION
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Paragraph 0593, (2020/05/02)
Provided are a curable composition, a cured film, an optical filter, a solid image pickup element, an image display device, an infrared sensor, a dispersing auxiliary agent, a dispersion, and a method of manufacturing a dispersion. With the curable composition, a cured film having excellent moisture resistance in which the formation of an aggregate derived from a compound having a colorant skeleton is suppressed can be formed. This curable composition includes: a compound A having a structure in which at least one functional group selected from an acid group having a pKa of 3 or lower and a Clog P value of ?1.1 or higher, an anionic group obtained by dissociating one or more hydrogen atoms from the acid group, or a salt of the acid group is bonded to a π-conjugated structure of a colorant skeleton and having a maximum absorption wavelength in a wavelength range of 650 to 1200 nm; a curable compound; and a solvent.
Facile net cycloaddition approach to optically active 1,5-benzothiazepines
Fukata, Yukihiro,Asano, Keisuke,Matsubara, Seijiro
supporting information, p. 5320 - 5323 (2015/05/13)
The 1,5-benzothiazepine moiety is well-known as a versatile pharmacophore, and its derivatives are expected to have antagonism against numerous diseases. Thus, it is desirable to develop a synthetic route that enables facile enantioselective preparation of a wide range of such derivatives. Although the cycloaddition approach could be considered a possible route to these compounds, to date, there has been no precedent of such a protocol. We therefore present the first example of a highly enantioselective net [4 + 3] cycloaddition to afford 1,5-benzothiazepines by utilizing α,β-unsaturated acylammonium intermediates generated by chiral isothiourea catalysts, which undergo two sequential chemoselective nucleophilic attacks by 2-aminothiophenols. This protocol provided cycloadducts in extremely high regioselectivity, with a good-to-excellent stereoselectivity being achieved regardless of the steric and electronic properties of the substrates. This method therefore offers promising synthetic routes for the construction of a library of optically active 1,5-benzothiazepines for assay evaluation.
DIHYDROBENZOFURAN DERIVATIVES AS INSECTICIDAL COMPOUNDS
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Page/Page column 125; 126, (2014/09/29)
Provided are compounds of formula (I) and methods of controlling insects, acarines, nematodes or molluscs, which comprises applying to a pest, to a locus of a pest, or to a plant susceptible to attack by a pest an insecticidally, acaricidally, nematicidally or molluscicidally effective amount of a compound of formula (I).
Pyridobenzothiazole derivatives as new chemotype targeting the HCV NS5B polymerase
Manfroni, Giuseppe,Meschini, Francesco,Barreca, Maria Letizia,Leyssen, Pieter,Samuele, Alberta,Iraci, Nunzio,Sabatini, Stefano,Massari, Serena,Maga, Giovanni,Neyts, Johan,Cecchetti, Violetta
experimental part, p. 866 - 876 (2012/03/13)
Hepatitis C virus (HCV) infection has been recognized as the major cause of liver failure that can lead to hepatocellular carcinoma. Among all the HCV proteins, NS5B polymerase represents a leading target for drug discovery strategies. Herein, we describe
11C-labelled PIB analogues as potential tracer agents for in vivo imaging of amyloid β in Alzheimer's disease
Serdons,Verduyckt,Vanderghinste,Borghgraef,Cleynhens,Van Leuven,Kung,Bormans,Verbruggen
experimental part, p. 1415 - 1426 (2009/07/04)
Pittsburgh Compound-B (PIB) is currently being evaluated clinically for in vivo visualization of amyloid plaques in patients with Alzheimer's disease (AD). We have synthesized three structural isomers of 6-hydroxy-2-(4′-aminophenyl)-1,3-benzothiazole, per
ISOTOPICALLY-LABELED BENZOTHIAZOLE COMPOUNDS AS IMAGING AGENTS FOR AMYLOIDOGENIC PROTEINS
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Page/Page column 52-53, (2008/06/13)
The present invention provides an isolated linezolid impurity, desfluoro linezolid, the preparation thereof and its use as a reference standard.
2-(Anilinomethyl)imidazolines as α1 adrenergic receptor agonists: The discovery of α10 subtype selective 2′-alkylsulfonyl-substituted analogues
Hodson, Stephen J.,Bishop, Michael J.,Speake, Jason D.,Navas III, Frank,Garrison, Deanna T.,Bigham, Eric C.,Saussy Jr., David L.,Liacos, James A.,Irving, Paul E.,Jeffrey Gobel,Sherman, Bryan W.
, p. 2229 - 2239 (2007/10/03)
A series of 2′-alkylthio-2-(anilinomethyl)imidazolines were prepared to examine the effect of the alkyl group size, sulfur oxidation state, and phenyl ring substitution on ligand binding and agonism of α-adrenergic receptor subtypes α1a, α1b, α1d, α2a, and α2c. Binding at all receptor subtypes decreased for compounds in the sulfone oxidation state as compared to their sulfide analogues. While sulfides were generally potent, nonselective agonists, sulfones exhibited α1a subtype selectivity in a cell-based functional assay. Sulfone (32) was 250-7000-fold selective for α1a vs all other subtypes.
Synthesis and biological evaluation of alkyl, alkoxy, alkylthio, or amino-substituted 2,3-dihydro-1,5-benzothiazepin-4(5H)-ones
Inoue, Hirozumi,Konda, Mikihiko,Hashiyama, Tomiki,Otsuka, Hisao,Watanabe, Akishige,Gaino, Mitsunori,Takahashi, Kaoru,Date, Tadamasa,Okamura, Kimio,Takeda, Mikio,Narita, Hiroshi,Murata, Sakae,Odawara, Akio,Sasaki, Haruhiko,Nagao, Taku
, p. 1008 - 1026 (2007/10/03)
2,3-Dihydro-1,5-benzothiazepin-4(5H)-ones substituted with an alkyl, alkoxy, alkylthio, hydroxy, or amino group on the fused benzene ring of the 1,5-benzothiazepine skeleton were synthesized and their vasodilating, antihypertensive, and platelet aggregation-inhibitory activities were investigated. (-)-cis-3-Acetoxy-5-[2-(dimethylamino)ethyl]-2,3-dihydro-8- methyl-2-(4-methylphenyl)-1,5-benzothiazepin-4(5H)-one ((-)-13e) was selected for further studies as a potent inhibitor of platelet aggregation.
