24248-74-6Relevant articles and documents
Parallel synthesis and biological evaluation of 5,6,7,8- tetrahydrobenzothieno[2,3-d]pyrimidin-4(3H)-one cytotoxic agents selective for p21-deficient cells
Jennings, Lee D.,Kincaid, Scott L.,Wang, Yanong D.,Krishnamurthy, Girija,Beyer, Carl F.,McGinnis, John P.,Miranda, Miriam,Discafani, Carolyn M.,Rabindran, Sridhar K.
, p. 4731 - 4735 (2007/10/03)
A novel series of inhibitors of cancer cell proliferation, selective against p21 cell cycle checkpoint-disrupted cells vs. cells with intact p21 checkpoint, were identified by high-throughput screening. Optimization of both ends of the lead molecule to improve potency, using parallel synthesis and iterative design, is described. The 2-(1,4-dibenzodioxane)-substituted derivative 14 was identified as a highly selective and potent agent displaying an IC50 of 91 nM in the p21-deficient cell line.
