1211757-83-3Relevant articles and documents
Pharmacologic inhibition of MNKs in acute myeloid leukemia
Teo, Theodosia,Lam, Frankie,Yu, Mingfeng,Yang, Yuchao,Basnet, Sunita K. C.,Albrecht, Hugo,Sykes, Matthew J.,Wang, Shudong
, p. 380 - 389 (2015)
The Ras/Raf/MAPK and PI3K/Akt/mTOR pathways are key signaling cascades involved in the regulation of cell proliferation and survival, and have been implicated in the pathogenesis of several types of cancers, including acute myeloid leukemia (AML). The onc
An integrated approach for discovery of highly potent and selective Mnk inhibitors: Screening, synthesis and SAR analysis
Teo, Theodosia,Yang, Yuchao,Yu, Mingfeng,Basnet, Sunita K.C.,Gillam, Todd,Hou, Jinqiang,Schmid, Raffaella M.,Kumarasiri, Malika,Diab, Sarah,Albrecht, Hugo,Sykes, Matthew J.,Wang, Shudong
, p. 539 - 550 (2015/10/12)
Deregulation of protein synthesis is a common event in cancer. As MAPK-interacting kinases (Mnks) play critical roles in regulation of protein synthesis, they have emerged as novel anti-cancer targets. Mnks phosphorylate eukaryotic initiation factor 4E (eIF4E) and promote eIF4E-mediated oncogenic activity. Given that the kinase activity of Mnks is essential for oncogenesis but is dispensable for normal development, the discovery of potent and selective pharmacological Mnk inhibitors provides pharmacological target validation and offers a new strategy for cancer treatment. Herein, comprehensive in silico screening approaches were deployed, and three thieno[2,3-d]pyrimidine and pyrazolo[3,4-d]pyrimidine derivatives were identified as hit compounds. Further chemical modification of thieno[2,3-d]pyrimidine derivative 3 has given rise to a series of highly potent Mnk2 inhibitors that could be potential leads for the treatment of acute myeloid leukemia.
THIENOPYRIMIDINES CONTAINING A SUBSTITUTED ALKYL GROUP FOR PHARMACEUTICAL COMPOSITIONS
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Page/Page column 68; 69, (2011/09/20)
The present invention relates to novel thienopyrimidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.