89322-66-7Relevant academic research and scientific papers
PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OF USE
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Page/Page column 201, (2008/12/06)
Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. [Insert Formula Ic and Id]
New base pairing motifs. The synthesis and thermal stability of oligodeoxynucleotides containing imidazopyridopyrimidine nucleosides with the ability to form four hydrogen bonds
Minakawa, Noriaki,Kojima, Naoshi,Hikishima, Sadao,Sasaki, Takashi,Kiyosue, Arihiro,Atsumi, Naoko,Ueno, Yoshihito,Matsuda, Akira
, p. 9970 - 9982 (2007/10/03)
The synthesis and thermal stability of oligodeoxynucleotides (ODNs) containing imidazo[5′,4′: 4,5]pyrido[2,3-d]pyrimidine nucleosides 1-4 (NN, OO, NO, and ON, respectively) with the aim of developing two sets of new base pairing motifs consisting of four hydrogen bonds (H-bonds) is described. The proposed four tricyclic nucleosides 1-4 were synthesized through the Stille coupling reaction of a 5-iodoimidazole nucleoside with an appropriate 5-stannylpyrimidine derivative, followed by an intramolecular cyclization. These nucleosides were incorporated into ODNs to investigate the H-bonding ability. When one molecule of the tricyclic nucleosides was incorporated into the center of each ODN (ODN I and II, each 17mer), no apparent specificity of base pairing was observed, and all duplexes were less stable than the duplexes containing natural G:C and A:T pairs. On the other hand, when three molecules of the tricyclic nucleosides were consecutively incorporated into the center of each ODN (ODN III and IV, each 17mer), thermal and thermodynamic stabilization of the duplexes due to the specific base pairings was observed. The melting temperature (Tm) of the duplex containing the NO:ON pairs showed the highest Tm of 84.0 °C, which was 18.2 and 23.5 °C higher than that of the duplexes containing G:C and A:T pairs, respectively. This result implies that NO and ON form base pairs with four H-bonds when they are incorporated into ODNs. The duplex containing NO:O N pairs was markedly stabilized by the assistance of the stacking ability of the imidazopyridopyrimidine bases. Thus, we developed a thermally stable new base pairing motif, which should be useful for the stabilization and regulation of a variety of DNA structures.
