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. 1977 Apr 15;196(4287):303-5.
doi: 10.1126/science.191910.

A phospholipid derivative of cytosine arabinoside and its conversion to phosphatidylinositol by animal tissue

C R Raetz, M Y Chu, S Srivastava, J G Turcotte

A phospholipid derivative of cytosine arabinoside and its conversion to phosphatidylinositol by animal tissue

C R Raetz et al. Science. .

Abstract

We have synthesized an analog (ara-CDP-DL-dipalmitin) of cytidine diphosphate diglyceride (CDP-diglyceride) in which the antitumor drug, cytosine arabinoside, is substituted for the cytidine moiety. Enzymes in rat and human liver convert this analog to phosphatidylinositol, thereby releasing cytosine arabinoside-5'-monophosphate, an obligatory intermediate in the activation of cytosine arabinoside. Unlike cytidine diphosphate diglyceride, however, ara-CDP-DL-diapalmitin is not an efficient substrate for phosphatidylglycerophosphate synthesis in liver or phosphatidylserine in Escherichia coli. The antitumor activity of ara-CDP-DL-dipalmitin in mice bearing L5178Y leukemia is described.

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