Nucleosides and nucleotides. 150. Enzymatic synthesis of 5′-phosphatidyl derivatives of 1-(2-C-cyano-2-deoxy-β-d-arabino-pentofuranosyl)cytosine (CNDAC (cas 135598-68-4)) and their notable antitumor effects in mice1

Add time:08/18/2019    Source:sciencedirect.com

1-(2-C-Cyano-2-deoxy-β-d-arabino-pentofuranosyl)cytosine (CNDAC, 1) is a potent antitumor nucleoside developed by us. A series of 5′-phosphatidyl derivatives of CNDAC bearing various fatty acyl residues, namely dimyristoyl derivative 3a, dipalmitoyl derivative 3b, distearoyl 3c, dioleoyl derivative 3d, and dilinoleoyl derivative 3e, was synthesized by phospholipase D-catalyzed transphosphatidylation. All of these 5′-phosphatidyl-CNDACs (3a-e) administered ip almost perfectly inhibited the growth of sc-implanted M5076 sarcoma in mice, and the effects were clearly superior to that of CNDAC.

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