88770-19-8Relevant academic research and scientific papers
Discovery of 6-substituted thieno[2,3-d]pyrimidine analogs as dual inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase in de novo purine nucleotide biosynthesis in folate receptor
Wallace-Povirk, Adrianne,Tong, Nian,Wong-Roushar, Jennifer,O'Connor, Carrie,Zhou, Xilin,Hou, Zhanjun,Bao, Xun,Garcia, Gloria E.,Li, Jing,Kim, Seongho,Dann, Charles E.,Matherly, Larry H.,Gangjee, Aleem
, (2021/03/29)
We discovered 6-substituted thieno[2,3-d]pyrimidine compounds (3–9) with 3–4 bridge carbons and side-chain thiophene or furan rings for dual targeting one-carbon (C1) metabolism in folate receptor- (FR) expressing cancers. Synthesis involved nine steps st
Thermal behaviour of dicarboxylic ester bithiophene polymers exhibiting a high open-circuit voltage
Heuvel, Ruurd,Colberts, Fallon J.M.,Wienk, Martijn M.,Janssen, René A.J.
, p. 3731 - 3742 (2018/04/12)
Nine different polythiophene derivatives based on dialkyl-(2,2′-bithiophene-5,5′-diyl)-4,4′-dicarboxylate (DCB) alternating with thiophene (T), bithiophene (2T) or thienothiophene (TT) as co-monomer have been synthesized to study the effect of the polymer backbone and side chain length on the thermal properties, the tendency to aggregate, and the photovoltaic performance. Polymers incorporating DCB and 2T show increased crystallinity and a large effect of the side chain length on the morphology of the photoactive layer blends. Thermal annealing increases the crystallinity of the polymers and enhances the long-wavelength light absorption. The concomitant increase in polymer fibre width, however, deteriorates the photovoltaic performance. The best devices were made using the PDCB-2T polymer with 2-butyloctyl side chains providing a power conversion efficiency of 5.18%. The PDCB-T polymer with 2-ethylhexyl substituents shows a comparable efficiency (5.08%), but with a significantly higher open-circuit voltage due to deeper frontier orbitals levels.
Macrocycles with bithiophene units: Synthesis, structure, and electrochemical properties
Dora Demeter,Claudia Lar,Jean Roncali,Grosu, Ion
, p. 1460 - 1462 (2013/05/08)
Bithiophene macrocycles with oligo(oxyethylene) loops were synthesized in good yields by reacting 4,40-bis(hydroxymethyl)-2,20-bithiophene with ditosylated oligoethyleneglycols. The structures of the macrocycles were elucidated by NMR spectroscopy and MS spectrometry. The electronic and electrochemical properties of the macrocyclic compounds were determined using cyclic voltammetry and UV-Vis spectroscopy. Copyright
(4-PHENYL-PIPERIDIN-1-YL)-[5-1H-PYRAZOL-4YL)-THIOPHEN-3-YL]-METHANONE COMPOUNDS AND THEIR USE
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Page/Page column 72, (2011/04/19)
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain (4-phenyl-piperidin-1-yl)- [5-(1 H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds that, inter alia, inhibit 11 β-hydroxysteroid dehydrogenase type 1 (11 β-HSD1 ). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 1 1 β-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11 β-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
FUSED HETEROCYCLYC INHIBITOR COMPOUNDS
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Page/Page column 110, (2010/03/02)
The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) and/or Cyclin-dependent kinase (CDK) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound
INDANE DERIVATES AS MUSCARINIC RECEPTOR AGONISTS
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Page 43-44, (2010/02/10)
The present invention relates to compounds of Formula I: I which are agonists of the M-1 muscarinic receptor.
Poly(alkyl thiophene-3-carboxylates). Synthesis, properties and electroluminescence studies of polythiophenes containing a carbonyl group directly attached to the ring
Pomerantz, Martin,Cheng, Yang,Kasim, Ramesh K.,Elsenbaumer, Ronald L.
, p. 2155 - 2163 (2007/10/03)
Improved synthetic methodology for poly(3-hexyl- and 3- octyloxycarbonylthiophene-2,5-diyl) (1a and 1b) is reported. M(n) = 6700 and 9400 (M(w)/M(n) = 2.5 and 3.2), λ(max) for fluorescence emission = 600 and 610 nm and λ(max) for electroluminescence = 600 and 615 nm, for 1a and 1b respectively. The 1H NMR spectra required that pentads be considered to explain the spectra. That is the four nearest neighbours to a given ring influence the 1H NMR spectrum. Electroluminescence efficiencies of 0.016% and 0.018% were observed for devices made from 1a and 1b, respectively. A bilayer device of ITO/poly(3-octylthiophene)/1b/A1 emitted at 646 nm, the same wavelength where poly(3-octylthiophene) itself emits. The efficiency was low but was an order of magnitude greater than for poly(3-octylthiophene) itself. Regioregular (HH-TT) poly(4,4'-bis(hexyl- and octyloxycarbonyl)[2,2'- bithiophene]-5,5'-diyl) (3a and 3b) were also prepared via the Ullmann reaction and M(n) = 7900 and 11000 respectively. Films of 3a and 3b were yellow in color and showed λ(max) = 377 and 381 nm respectively, about 55-80 nm blue shifted compared with 1a and 1b. This is due to the large rotational barrier in the HH dyads which reduces the effective conjugation length in 3a and 3b. 3a and 3b showed bright fluorescence and electroluminescence with emission of yellow light. Electroluminescence efficiencies were 8.5 x 10-3% and 4.7 x 10-3%, respectively.
Synthesis and antitumour activity of new derivatives of flavone-8- acetic acid (FAA). Part 31): 2-Heteroaryl derivatives
Aitken, R. Alan,Bibby, Michael C.,Bielefeldt, Florian,Double, John A.,Laws, Andrea L.,Mathieu, Anne-Laure,Ritchie, Robert B.,Wilson, David W. J.
, p. 405 - 411 (2007/10/03)
A range of 14 derivatives of flavone-8-acetic acid (FAA) with a heterocyclic substituent in place of the 2-phenyl group have been prepared and their anti-tumour activity evaluated in vitro against a panel of human and murine tumour cell lines and in vivo against MAC 15A. Some of the compounds, notably 2c,d and s, showed significant in vivo activity and these require further studies in order to evaluate their potential for development.
