Anti-cancer ProTides: tuning the activity of BVDU phosphoramidates related to thymectacin

C McGuigan, JC Thiery, F Daverio, WG Jiang…

Index: McGuigan, Christopher; Thiery, Jean-Christophe; Daverio, Felice; Jiang, Wen G.; Davies, Gaynor; Mason, Malcolm Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 9 p. 3219 - 3227

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Citation Number: 46

Abstract

Based on our wide ranging knowledge of phosphoramidate ProTides as anti-viral agents we have tuned the lead anti-cancer agent thymectacin in the ester and amino acid regions and revealed a substantial enhancement in in vitro potency versus colon and prostate cancer cell lines. Twelve analogues have been reported, with yields of 29–78%. The compounds are fully characterised and data clearly reveal the presence of two phosphate ...