502145-83-7Relevant 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).
