The antiproliferative activity of 9-β-d-arabinofuranosyladenine 5′-monophosphate against a cultured line of mouse leukemia cells (L1210/C2) was enhanced by addition of either 2′-deoxycoformycin or erythro-9-(2-hydroxy-3-nonyl)adenine. The activity of 9-β-d-arabinofuranosyladenine 5′-monophosphate, alone or in combination with either of the two inhibitors of adenosine deaminase, was comparable to that of 9-β-d-arabinofuranosyladenine (ara-A), apparently reflecting the rapid conversion of 9-β-d-arabinofuranosyladenine 5′-monophosphate to ara-A by L1210/C2 cells. Several ara-A analogs were assayed for antiproliferative activity against L1210/C2 cells; of these, only 9-β-d-arabinofuranosyladenine 5′-O-methylphosphate and 2′-deoxy-2′-amino-9-β-d-arabinofuranosyladenine were active. Addition of 2′-deoxycoformycin to cell culture fluids enhanced the activity of 9-β-d-arabinofuranosyladenine 5′-O-methylphosphate suggesting conversion to an adenosine deaminase-sensitive intermediate, presumably ara-A.

1

Supported by the National Cancer Institute of Canada.

This content is only available via PDF.