310400-99-8Relevant academic research and scientific papers
Development of potent purine-derived nitrile inhibitors of the trypanosomal protease TbcatB
Mallari, Jeremy P.,Shelat, Anang A.,Obrien, Terri,Caffrey, Conor R.,Kosinski, Aaron,Connelly, Michele,Harbut, Michael,Greenbaum, Doron,McKerrow, James H.,Guy, R. Kiplin
, p. 545 - 552 (2008/09/18)
Human African trypanosomiasis (HAT), a major health concern in sub-Saharan Africa, is caused by the protozoan parasite Trypanosoma brucei. Recent studies have shown that a cathepsin B like protease, TbcatB, is essential to the survival of T. brucei in vit
Derivatives of purine, their preparation process and pharmaceutical compositions containing them
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Page/Page column 16, (2010/02/13)
A compound of the formula wherein R is defined as in the specification, which compounds have an inhibitory effect vis-à-vis cycline-dependent kinase proteins (cdk) and are endowed with antimitotic properties.
6,9-DISUBSTITUTED 2- TRANS-(4- AMINOCYCLOHEXYL) AMINO]PURINES
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Page 32, (2008/06/13)
The present invention provides novel compounds of formula (I) wherein R is selected from the group consisting of R2, R2NH-, or H2N-R3- wherein R2 is selected from the group consisting of C1-C8 alkyl and formula (II), wherein Z is selected from the group c
6,9,-disubstituted 2-[trans-(4-aminocyclohexyl) amino] purines
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, (2008/06/13)
The present invention provides novel compounds of the formula (I) wherein R is selected from the group consisting of R2, R2NH—, or H2N—R3— wherein R2 is selected from the group consisting of C1-C8alkyl and ?wherein Z is selected from the group consisting of phenyl, heterocycle and cycloalkyl, each R4 is independently hydrogen or C1-C4alkyl, and n is an integer 1-8; wherein each C1-C8alkyl and Z is optionally substituted with 1 to 3 substituents, which may be the same or different, selected from the group consisting of Ha1, OH, and C1-C4alkyl; R3 is C1-C8alkylene; and R1 is selected from the group consisting of cyclopentyl and isopropyl, and the pharmaceutically acceptable salts, optical isomers, and hydrates thereof. In addition, the present invention provides a method of inhibiting cell cycle progression. More specifically, the present invention provides a method of inhibiting cyclin dependent kinases, particularly cdk-2. The present invention also provides a method of preventing apoptosis in neuronal cells and a method of inhibiting the development of neoplasms. In addition, the present invention provides a composition comprising an assayable amount of a compound of Formula (I) in admixture or otherwise in association with an inert carrier. The present invention also provides a pharmaceutical composition comprising an effective inhibitory amount of a compound of Formula (I) in admixture or otherwise in association with one or more pharmaceutically acceptable carriers or excipients.
Crystal structure of human cyclin-dependent kinase 2 in complex with the adenine-derived inhibitor H717
Dreyer,Borcherding,Dumont,Peet,Tsay,Wright,Bitonti,Shen,Kim
, p. 524 - 530 (2007/10/03)
Cyclin-dependent kinases (CDKs) are regulatory proteins of the eukaryotic cell cycle. They act after association with different cyclins, the concentrations of which vary throughout the progression of the cell cycle. As central mediators of cell growth, CD
