336115-13-0Relevant academic research and scientific papers
Fluorinated quinazolinones as potential radiotracers for imaging kinesin spindle protein expression
Holland, Jason P.,Jones, Michael W.,Cohrs, Susan,Schibli, Roger,Fischer, Eliane
, p. 496 - 507 (2013/03/13)
Anti-mitotic anti-cancer drugs offer a potential platform for developing new radiotracers for imaging proliferation markers associated with the mitosis-phase of the cell-cycle. One interesting target is kinesin spindle protein (KSP) - an ATP-dependent motor protein that plays a vital role in bipolar spindle formation. In this work we synthesised a range of new fluorinated-quinazolinone compounds based on the structure of the clinical candidate KSP inhibitor, ispinesib, and investigated their properties in vitro as potential anti-mitotic agents targeting KSP expression. Anti-proliferation (MTT and BrdU) assays combined with additional studies including fluorescence-assisted cell sorting (FACS) analysis of cell-cycle arrest confirmed the mechanism and potency of these biphenyl compounds in a range of human cancer cell lines. Additional studies using confocal fluorescence microscopy showed that these compounds induce M-phase arrest via monoaster spindle formation. Structural studies revealed that compound 20-(R) is the most potent fluorinated-quinazolinone inhibitor of KSP and represents a suitable lead candidate for further studies on designing 18F-radiolabelled agents for positron-emission tomography (PET).
Imides: Forgotten players in the Ugi reaction. One-pot multicomponent synthesis of quinazolinones
Mossetti, Riccardo,Pirali, Tracey,Saggiorato, Desiree,Tron, Gian Cesare
, p. 6966 - 6968 (2011/08/21)
Up to now, the synthesis of quinazolinones has required lengthy synthetic procedures. Here, we describe an innovative one-pot multicomponent reaction leading to highly substituted quinazolinones. We believe that this novel transformation may open the door
