13455-81-7Relevant academic research and scientific papers
Amine-functionalized Metal-Organic Frameworks: An Efficient and Recyclable Heterogeneous Catalyst for the Knoevenagel Condensation Reaction
Taher, Abu,Lee, Dong-Jin,Lee, Byoung-Ki,Lee, Ik-Mo
, p. 1433 - 1437 (2016)
A highly efficient and reusable catalyst based on metal-organic frameworks (MOF) has been synthesized by post-functionalization and applied in Knoevenagel condensations of various aldehydes and ketones. The catalytic efficiency was demonstrated by the hig
Base-mediated benzannulation of α-cyanocrotonates with ynones: Facile synthesis of benzonitriles and fluorenes
Maddi, Sridhar Reddy,Nagireddy, Attunuri,Singam, Maneesh Kumar Reddy
, p. 2370 - 2374 (2020)
Here, we have demonstrated a strategic rapid approach for the synthesis of benzonitriles and cyanofluorenes via the [3 + 3] benzannulation of readily available alkynones and α-cyanocrotonates, a protocol par excellence for aryl nitriles. This decarboxylat
A facile microwave-assisted Knoevenagel condensation of various aldehydes and ketones using amine-functionalized metal organic frameworks
Lee, Ik-Mo,Lumbiny, Bilkis Jahan,Taher, Abu
, (2020/07/16)
An amine-functionalized metal organic framework (MOF) was used as highly efficient and recyclable heterogeneous catalyst for Knoevenagel condensation of various aromatic aldehydes and ketones in ethanol. The catalytic efficiency was demonstrated by the hi
Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2- d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors
Romagnoli, Romeo,Prencipe, Filippo,Oliva, Paola,Baraldi, Stefania,Baraldi, Pier Giovanni,Schiaffino Ortega, Santiago,Chayah, Mariem,Kimatrai Salvador, Maria,Lopez-Cara, Luisa Carlota,Brancale, Andrea,Ferla, Salvatore,Hamel, Ernest,Ronca, Roberto,Bortolozzi, Roberta,Mariotto, Elena,Mattiuzzo, Elena,Viola, Giampietro
supporting information, p. 1274 - 1290 (2019/01/30)
The clinical evidence for the success of tyrosine kinase inhibitors in combination with microtubule-targeting agents prompted us to design and develop single agents that possess both epidermal growth factor receptor (EGFR) kinase and tubulin polymerization inhibitory properties. A series of 6-aryl/heteroaryl-4-(3′,4′,5′-trimethoxyanilino)thieno[3,2-d]pyrimidine derivatives were discovered as novel dual tubulin polymerization and EGFR kinase inhibitors. The 4-(3′,4′,5′-trimethoxyanilino)-6-(p-tolyl)thieno[3,2-d]pyrimidine derivative 6g was the most potent compound of the series as an antiproliferative agent, with half-maximal inhibitory concentration (IC50) values in the single- or double-digit nanomolar range. Compound 6g bound to tubulin in the colchicine site and inhibited tubulin assembly with an IC50 value of 0.71 μM, and 6g inhibited EGFR activity with an IC50 value of 30 nM. Our data suggested that the excellent in vitro and in vivo profile of 6g may be derived from its dual inhibition of tubulin polymerization and EGFR kinase.
Synthesis and antimicrobial activity of novel 2-(pyridin-2-yl)thieno[2,3-d] pyrimidin-4 (3H)-ones
Haswani, Nitin G.,Bari, Sanjaykumar B.
experimental part, p. 915 - 924 (2012/02/16)
In the present study, some new 2-(pyridin-2-yl)thieno[2,3-d]pyrimidin-4(3H) -ones derivatives (IIa-o) were synthesized. The target compounds (IIa-o) were synthesized through the acid catalyzed condensation of 2-cyano, 3-cyano, and 4-cyano-pyridines with various 2-amino-3-carbethoxythiophenes (Ia-e). All thiophene derivatives were synthesized by Gewald reaction. The structures of the newly synthesized compounds were confirmed by UV-Visible, FT-IR, 1H-NMR, and mass spectral studies. All synthesized compounds were evaluated for their antimicrobial activity against various gram-positive and gram-negative bacterial and fungal strains. Amongst the synthesized compounds IIa, IIb, IId, IIe, and IIm were found to be active. TUeBITAK.
THIENOPYRIMIDINE DERIVATIVES AS POTASSIUM CHANNEL INHIBITORS
-
Page 28, (2008/06/13)
The present invention provides thienopyrimidine compounds which are potasium channels inhibitors. Pharmaceutical compositions comprising the compounds and their use in the treatment of arrhythmia are also provided.
Indeno[1,2-b]pyrazin-2,3-diones: A new class of antagonists at the glycine site of the NMDA receptor with potent in vivo activity
Jimonet, Patrick,Ribeill, Yves,Bohme, Georg Andrees,Boireau, Alain,Chevé, Michel,Damour, Dominique,Doble, Adam,Genevois-Borella, Arielle,Herman, Frédéric,Imperato, Assunta,Le Guern, Sylvain,Manfré, Franco,Pratt, Jeremy,Randle, John C. R.,Stutzmann, Jean-Marie,Mignani, Serge
, p. 2371 - 2381 (2007/10/03)
Indeno[1,2-b]pyrazin-2,3-diones have been identified as a novel series of potent ligands on the glycine site of the NMDA receptor. To improve their in vivo activities, an acetic acid-type side chain was introduced to the 5- position, giving water-soluble
