190973-16-1Relevant academic research and scientific papers
Bioactivity of glycogen phosphorylase inhibitors that bind to the purine nucleoside site
Hampson, Laura J.,Arden, Catherine,Agius, Loranne,Ganotidis, Minas,Kosmopoulou, Magda N.,Tiraidis, Costas,Elemes, Yiannis,Sakarellos, Constantinos,Leonidas, Demetres D.,Oikonomakos, Nikos G.
, p. 7835 - 7845 (2006)
The bioactivity in hepatocytes of glycogen phosphorylase inhibitors that bind to the active site, the allosteric activator site and the indole carboxamide site has been described. However, the pharmacological potential of the purine nucleoside inhibitor s
Identification of a new series of flavopiridol-like structures as kinase inhibitors with high cytotoxic potency
Alami, Mouad,Bach, Stéphane,Bignon, Jerome,Bonnet, Pascal,Brion, Jean-Daniel,Colas, Pierre,Hamze, Abdallah,Ibrahim, Nada,Josselin, Béatrice,Levaique, Helene,Messaoudi, Samir,Peyrat, Jean-Fran?ois,Robert, Thomas
, (2020)
In this work, unique flavopiridol analogs bearing thiosugars, amino acids and heterocyclic moieties tethered to the flavopiridol via thioether and amine bonds mainly on its C ring have been prepared. The analogs bearing thioether-benzimidazoles as substituents have demonstrated high cytotoxic activity in vitro against up to seven cancer cell lines. Their cytotoxic effects are comparable to those of flavopiridol. The most active compound 13c resulting from a structure-activity relationship (SAR) study and in silico docking showed the best antiproliferative activity and was more efficient than the reference compound. In addition, compound 13c showed significant nanomolar inhibition against CDK9, CDK10, and GSK3β protein kinases.
Structure-activity relationship studies of flavopiridol analogues
Murthi, Krishna K.,Dubay, Marja,McClure, Christopher,Brizuela, Leonardo,Boisclair, Michael D.,Worland, Peter J.,Mansuri, Muzammil M.,Pal, Kollol
, p. 1037 - 1041 (2007/10/03)
Cyclin dependent kinases (CDKs) along with the complementary cyclins form key regulatory checkpoint controls on the cell cycle. Flavopiridol is a synthetic flavone that shows potent and selective cyclin-dependent kinase inhibitory activity. In this paper, we report modifications of the 3-hydroxy-1-methylpiperidinyl (D ring) of flavopiridol and their effect on CDK inhibitory activity. (C) 2000 Elsevier Science. All rights reserved.
