Synthesis and evaluation of phosphorus containing, specific CDK9/CycT1 inhibitors

…, Z Greff, A Sipos, Z Varga, R Székely…

Index: Nemeth, Gabor; Greff, Zoltan; Sipos, Anna; Varga, Zoltan; Szekely, Rita; Sebestyen, Monika; Jaszay, Zsuzsa; Beni, Szabolcs; Nemes, Zoltan; Pirat, Jean-Luc; Volle, Jean-Noel; Virieux, David; Gyuris, Agnes; Kelemenics, Katalin; Ay, Eva; Minarovits, Janos; Szathmary, Susan; Keri, Gyoergy; Orfi, Laszlo Journal of Medicinal Chemistry, 2014 , vol. 57, # 10 p. 3939 - 3965

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Citation Number: 21

Abstract

Although there is a significant effort in the design of a selective CDK9/CycT1 inhibitor, no compound has been proven to be a specific inhibitor of this kinase so far. The aim of this research was to develop novel and selective phosphorus containing CDK9/CycT1 inhibitors. Molecules bearing phosphonamidate, phosphonate, and phosphinate moieties were synthesized. Prepared compounds were evaluated in an enzymatic CDK9/CycT1 assay. ...