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6-[1-(2,6-Difluorophenyl)ethyl]pyrimidinones Antagonize Cell Proliferation and Induce Cell Differentiation by Inhibiting (a Nontelomeric) Endogenous Reverse Transcriptase

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posted on 2005-11-03, 00:00 authored by Sara Bartolini, Antonello Mai, Marino Artico, Nicola Paesano, Dante Rotili, Corrado Spadafora, Gianluca Sbardella
Two 2,6-difluoro-DABO derivatives (MC 1047, 1, and MC 1220, 2, respectively) were tested against endogenous, nontelomeric reverse transcriptase (endo-RT) in human differentiating cell systems to investigate their antiproliferative and cytodifferentiating activity. The two compounds significantly reduced cell proliferation and facilitated the morphological differentiation of cells. These results propose F2-DABOs as useful tools in preventive and/or curative therapy to counteract the loss of differentiation in dedifferentiating pathologies and as antiproliferative drugs in tumor therapy.

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