1595282-82-8Relevant academic research and scientific papers
Synthesis and biological evaluation of selected 7H-pyrrolo[2,3-d]pyrimidine derivatives as novel CDK9/CyclinT and Haspin inhibitors
Pieterse, Lianie,Beteck, Richard M.,Baratte, Blandine,Jesumoroti, Omobolanle J.,Robert, Thomas,Ruchaud, Sandrine,Bach, Stéphane,Legoabe, Lesetja J.
, (2021)
Protein kinases, including CDK9/CyclinT and Haspin, are regarded as potential drug targets in cancer therapy. Findings from a previous study suggested 7-azaindole as a privileged scaffold for producing inhibitors of CDK9/CyclinT and Haspin. Inspired by these findings, the current study synthesised and evaluated thirteen (13) C6-substituted 7-azaindole and twenty (20) C4-substituted structurally related 7H-pyrrolo[2,3-d]pyrimidine derivatives against a panel of protein kinases, including CDK9/CyclinT and Haspin. Eleven of the 7H-pyrrolo[2,3-d]pyrimidine derivatives exhibited activity toward CDK9/CyclinT, while 4 of compounds had activity against Haspin. The best CDK9/CyclinT (IC50 of 0.38 μM) and Haspin (IC50 of 0.11 μM) activities were achieved by compounds 7d and 7f, respectively. Hence, these compounds may be valuable starting points for development of new anti-cancer drugs.
Using 'biased-privileged' scaffolds to identify lysine methyltransferase inhibitors
Kashyap, Sudhir,Sandler, Joel,Peters, Ulf,Martinez, Eduardo J.,Kapoor, Tarun M.
supporting information, p. 2253 - 2260 (2014/04/17)
Methylation of histones by lysine methyltransferases (KMTases) plays important roles in regulating chromatin function. It is also now clear that improper KMTases activity is linked to human diseases, such as cancer. We report an approach that employs drug
