384850-37-7Relevant articles and documents
Synthesis of poly(1-chloro-2-arylacetylene)s with high cis-content and examination of their absorption/emission properties
Rodriguez Castanon, Jesus,Sano, Natsuhiro,Shiotsuki, Masashi,Sanda, Fumio
, p. 382 - 388 (2017)
A series of 1-chloro-2-arylacetylenes [Cl-C?C-Ar, Ar = C6H5 (1), C6H4-p-iPr (2), C6H4-p-OiPr (3), C6H4-p-NHC(O)OtBu (4), and C6H4-o-iPr (5)] were polymerized using (tBu3P)PdMeCl/silver trifluoromethanesulfonate (AgOTf) and MoCl5/SnBu4 catalysts. The corresponding polymers [poly(1)–poly(5)] with weight-average molecular weights of 6,500–690,000 were obtained in 10–91% yields. THF-insoluble parts, presumably high-molecular weight polymers, were formed together with THF-soluble polymers by the Pd-catalyzed polymerization. The Pd catalyst polymerized nonpolar monomers 1 and 2 to give the polymers in yields lower than the Mo catalyst, while the Pd catalyst polymerized polar monomers 3 and 4 to give the corresponding polymers in higher yields. The 1H NMR and UV–vis absorption spectra of the polymers indicated that the cis-contents of the Pd-based polymers were higher than those of the Mo-based polymers, and the conjugation length of the Pd-based polymers was shorter than that of the Mo-based polymers. Pd-based poly(5) emitted fluorescence most strongly among poly(1)–poly(5).
4-Amino-5-aryl-6-arylethynylpyrimidines: Structure-activity relationships of non-nucleoside adenosine kinase inhibitors
Matulenko, Mark A.,Paight, Ernest S.,Frey, Robin R.,Gomtsyan, Arthur,DiDomenico Jr., Stanley,Jiang, Meiqun,Lee, Chih-Hung,Stewart, Andrew O.,Yu, Haixia,Kohlhaas, Kathy L.,Alexander, Karen M.,McGaraughty, Steve,Mikusa, Joseph,Marsh, Kennan C.,Muchmore, Steven W.,Jakob, Clarissa L.,Kowaluk, Elizabeth A.,Jarvis, Michael F.,Bhagwat, Shripad S.
, p. 1586 - 1605 (2008/02/01)
A series of non-nucleoside adenosine kinase (AK) inhibitors is reported. These inhibitors originated from the modification of 5-(3-bromophenyl)-7-(6-morpholin-4-ylpyridin-3-yl)pyrido[2,3-d]pyrimidin-4-ylamine (ABT-702). The identification of a linker that would approximate the spatial arrangement found between the pyrimidine ring and the aryl group at C(7) in ABT-702 was a key element in this modification. A search of potential linkers led to the discovery of an acetylene moiety as a suitable scaffold. It was hypothesized that the aryl acetylenes, ABT-702, and adenosine bound to the active site of AK (closed form) in a similar manner with respect to the orientation of the heterocyclic base. Although potent acetylene analogs were discovered based on this assumption, an X-ray crystal structure of 5-(4-dimethylaminophenyl)-6-(6-morpholin-4-ylpyridin-3-ylethynyl)pyrimidin-4-ylamine (16a) revealed a binding orientation contrary to adenosine. In addition, this compound bound tightly to a unique open conformation of AK. The structure-activity relationships and unique ligand orientation and protein conformation are discussed.
5,6,7-trisubstituted-4-aminopyrido[2,3-D] pyrimidine compounds
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, (2008/06/13)
A compound having the formula wherein R1, R2, R3, R4 and R5 are defined, a method for inhibiting adenosine kinase by administering a compound thereof, a pharmaceutical composition comprising a therapeutically effective amount of a compound thereof above i