83726-75-4Relevant academic research and scientific papers
Synthesis and antitumor activity of bithienyl-pyrimidine derivatives with electrostatic binding side chains
Chou, Yi-Meen,Lai, Ming Chih,Hwang, Tsai-Mian,Ong, Chi Wi
, p. 2643 - 2646 (1999)
A series of bithienyl-pyrimidines having cationic side chain have been developed as antitumor agents. This work illustrates the overwhelming importance of the bithienyl unit for efficient DNA binding. The X-ray structure of 4-(2',2'-thien-5-yl)-2-chloropyrimidine was obtained for postulating the conformation of the bithienyl-pyrimidine moiety.
METHODS AND COMPOSITIONS OF INHIBITING DCN1-UBC12 INTERACTION
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Paragraph 00470, (2017/04/11)
In one aspect, the invention relates to substituted l-phenyl-3-(piperidin-4-yl)urea analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the DCN1-UBC12 interaction inhibitors of DCN1 -mediated cullin-RING ligase activity, methods of making same, pharmaceutical compositions comprising same, methods of treating disorders using the disclosed compounds and compositions, methods of treating disorders associated with a DCN1-UBC12 interaction dysfunction, methods of treating disorders associated with a DCN1-mediated cullin-RING ligase activity dysfunction, methods of male contraception comprising the disclosed compounds and compositions, and kits comprising the disclosed compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
NOVEL OXAZOLE DERIVATIVES THAT INHIBIT SYK
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Paragraph 0106, (2017/04/04)
The present invention is concerned with substituted oxazole derivatives that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant protein kinases implicated in a variety of human and animal diseases s
Synthesis and structure-activity relationship analysis of 5-HT7 receptor antagonists: Piperazin-1-yl substituted unfused heterobiaryls
Strekowski, Lucjan,Saczewski, Jaros?aw,Raux, Elizabeth A.,Fernando, Nilmi T.,Klenc, Jeff,Paranjpe, Shirish,Raszkiewicz, Aldona,Blake, Ava L.,Ehalt, Adam J.,Barnes, Samuel,Baranowski, Timothy C.,Sullivan, Shannon M.,Sata?a, Grzegorz,Bojarski, Andrzej J.
, (2016/05/24)
A series of piperazin-1-yl substituted unfused heterobiaryls was synthesized as ligands of the 5-HT7 receptors. The goal of this project was to elucidate the structural features that affect the 5-HT7 binding affinity of this class of compounds represented by the model ligand 4-(3-furyl)-2-(4-methylpiperazin-1-yl)pyrimidine (2). The SAR studies included systematical structural changes of the pyrimidine core moiety in 2 to quinazoline, pyridine and benzene, changes of the 3-furyl group to other heteroaryl substituents, the presence of various analogs of the 4-methylpiperazin-1-yl group, as well as additional substitutions at positions 5 and 6 of the pyrimidine. Substitution of position 6 of the pyrimidine in the model ligand with an alkyl group results in a substantial increase of the binding affinity (note a change in position numbers due to the nomenclature rules). It was also demonstrated that 4-(3-furyl) moiety is crucial for the 5-HT7 binding affinity of the substituted pyrimidines, although, the pyrimidine core can be replaced with a pyridine ring without a dramatic loss of the binding affinity. The selected ethylpyrimidine (12) and butylpyrimidine (13) analogs of high 5-HT7 binding affinity showed antagonistic properties in cAMP functional test and varied selectivity profile-compound 12 can be regarded as a dual 5-HT7 /5-HT2A R ligand, and 13 as a multi-receptor (5-HT7 , 5-HT2A , 5-HT6 and D2 ) agent.
DIAZASPIROALKANEONE-SUBSTITUTED OXAZOLE DERIVATIVES AS SPLEEN TYROSINE KINASE INHIBITORS
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Page/Page column 39; 40, (2015/12/08)
The present invention is concerned with diazaspiroalkanone- substituted oxazole derivatives that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant protein kinases implicated in a variety of human a
COMPOUNDS THAT INDUCE PANCREATIC BETA-CELL EXPANSION
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Page/Page column 9, (2010/06/14)
The present invention relates to compounds and compositions for inducing the expansion of pancreatic β-cells. The invention further relates to a use of these expanded pancreatic β-cells to reversibly expand pancreatic β-cells and other quiescent cells to overcome deficits associated with degenerative and/or autoimmune diseases.
Palladium-catalyzed cross-couplings of lithium arylzincates with aromatic halides: Synthesis of analogues of isomeridianin G and evaluation as GSK-3β inhibitors
Seggio, Anne,Priem, Ghislaine,Chevallier, Floris,Mongin, Florence
experimental part, p. 3617 - 3632 (2010/03/05)
Several analogues of isomeridianin G have been synthesized using palladium-catalyzed cross-coupling reactions of lithium triorganozincates as a key step. The latter have been prepared by deprotonative lithiation followed by transmetalation using ZnCl
Substituted nitrogen-containing heteroaryl derivatives useful as modulators of the histamine H4 receptor
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Page/Page column 52, (2009/04/24)
The present invention relates to substituted nitrogen-containing heteroaryl derivatives, pharmaceutical compositions containing them, and methods of using any of these derivatives and compositions for H4 receptor activity modulation and the tre
Synthesis of unsymmetrical heterobiaryls using palladium-catalyzed cross-coupling reactions of lithium organozincates
Seggio, Anne,Jutand, Anny,Priem, Ghislaine,Mongin, Florence
experimental part, p. 2955 - 2960 (2009/06/27)
Several unsymmetrical heterobiaryls have been synthesized through palladium-catalyzed cross-coupling reactions of lithium triorganozincates. The latter have been prepared by deprotonative lithiation followed by transmetalation using non-hygroscopic ZnCl2-TMEDA (0.33 equiv). Georg Thieme Verlag Stuttgart.
Inhibitors of Hepatitis C Virus
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Page/Page column 65, (2008/12/04)
Macrocyclic peptides are disclosed having the general formula: wherein R3, R3′, R4, R6, R′, X, Q and W are described. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
