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An In Vitro Enzymatic Assay to Measure Transcription Inhibition by Gallium(III) and H3 5,10,15-tris(pentafluorophenyl)corroles
Published on: March 18, 2015
Fluorocyclopentenyl-cytosine with broad spectrum and potent antitumor activity
Won Jun Choi1, Hwa-Jin Chung, Girish Chandra
1Department of Bioinspired Science and College of Pharmacy, Ewha Womans University, Seoul 120-750, Korea.
Abstract:
On the basis of the potent biological activity of cyclopentenyl-pyrimidines, fluorocyclopentenyl-pyrimidines were designed and synthesized from D-ribose. Among these, the cytosine derivative 5a showed highly potent antigrowth effects in a broad range of tumor cell lines and very potent antitumor activity in a nude mouse tumor xenograft model implanted with A549 human lung cancer cells. However, its 2'-deoxycytidine derivative 5b did not show any antigrowth effects, indicating that 2'-hydroxyl group is essential for the biological activity.
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