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New Neplanocin Analogues II. Enzymatic One-Step Synthesis and Antitumor Activity of 6′-(3-sn-Phosphatidyl)Neplanocin a Derivatives
Authors:Satoshi Shuto  Hiromichi Ito  Takumi Obara  Keiji Nakagami  Masao Yaso  Satoshi Yaginuma
Institution:Research Laboratories , Toyo Jozo Co., Ltd. , 632-1 Mifuku, Ohito-cho, Tagata-gun, Shizuoka, 410-23, Japan
Abstract:Abstract

A novel series of neplanocin analogues, 6′-(3-sn-phosphatidyl)neplanocin As bearing a variety of fatty acyl or alkyl residues in the glyceride moiety (2b-2h), were synthesized by means of phospholipase D-catalyzed transphosphatidylation. Among them, 2b, 2c, and 2e each exhibited significant antitumor effect against P388 leukemia in mice, which evidently surpassed that of parent compound neplanocin A.
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