1283119-10-7Relevant academic research and scientific papers
PIPERAZINYLPYRIMIDINE ANALOGUES AS PROTEIN KINASE INHIBITORS
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Page/Page column 16, (2012/03/12)
The invention provides novel compounds based on piperazinylpyrimidine derivatives to be used as protein kinase inhibitors. The compounds may be useful in treating or preventing different cellular proliferation disorders, such as cancer. The present invent
Anti-tumor pyrimidinylpiperazines bind to the prosurvival Bcl-2 protein family member Bcl-XL
Shallal, Hassan M.,Faridi, Jesika S.,Russu, Wade A.
body text, p. 1325 - 1328 (2011/04/16)
Overexpression of prosurvival or underexpression of pro-death Bcl-2 family proteins can lead to cancer cell resistance to chemotherapy and radiation treatment. Inhibition of the prosurvival Bcl-2 family proteins has become a strategy for cancer therapy and inhibitors are currently being evaluated in the clinic both as single agents and in combination with established drugs. Here we describe the design, synthesis, and evaluation of pyrimidylpiperazines that were discovered to be inhibitors of the prosurvival Bcl-2 protein family member Bcl-XL. This study identified compound 21 which demonstrated a GI50 value of 8.4 μM against A549 lung adenocarcinoma cells and a binding affinity Ki value for Bcl-XL of 127 nM.
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives
Shallal, Hassan M.,Russu, Wade A.
, p. 2043 - 2057 (2011/06/21)
Protein kinases play several pertinent roles in cell proliferation, and targeting these proteins has been shown to be a successful strategy toward controlling different malignancies. Despite the great discovery stories during the last two decades, there i
