294647-87-3Relevant academic research and scientific papers
Biaryl purine derivatives as potent antiproliferative agents: Inhibitors of cyclin dependent kinases. Part I
Trova, Michael P.,Barnes, Keith D.,Barford, Curt,Benanti, Travis,Bielaska, Mark,Burry, Lori,Lehman, John M.,Murphy, Christine,O'Grady, Harold,Peace, Denise,Salamone, Susan,Smith, Jennifer,Snider, Patricia,Toporowski, Joseph,Tregay, Steven,Wilson, Alison,Wyle, Michael,Zheng, Xiaozhang,Friedrich, Thomas D.
scheme or table, p. 6608 - 6612 (2010/06/12)
The introduction of an aryl ring onto the 4-position of the C-6 benzyl amino group of the Cdk inhibitor roscovitine (2), maintained the potent Cdk inhibition demonstrated by roscovitine (2) as well as greatly improving the antiproliferative activity. A series of C-6 biarylmethylamino derivatives was prepared addressing modifications on the C-6 biaryl rings, N-9 and C-2 positions to provide compounds that displayed potent cytotoxic activity against tumor cell lines. In particular, derivative 21h demonstrated a >750-fold improvement in the growth inhibition of HeLa cells compared to roscovitine (2).
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
Synthesis and activity of 2,6,9-trisubstituted purines
Schow, Steven R.,Mackman, Richard L.,Blum, Cheri L.,Brooks, Eric,Horsma, Amy G.,Joly, Alison,Kerwar, Suresh S.,Lee, Gavin,Shiffman, Dov,Nelson, Marek G.,Wang, Xingbo,Wick, Michael M.,Zhang, Xiaoming,Lum, Robert T.
, p. 2697 - 2702 (2007/10/03)
The preparation of a series of 2,6,9-trisubstituted purines and the structure-activity data for the inhibition of cyclin dependent kinase, CDK2 are presented.
