Nucleosides and nucleotides. 83. Design, synthesis, and antineoplastic activity of 2'-deoxy-2'-methylidenecytidine

K Takenuki, A Matsuda, T Ueda, T Sasaki…

Index: Takenuki, Kenji; Matsuda, Akira; Ueda, Tohru; Sasaki, Takuma; Fujii, Akihiro; Yamagami, Keiji Journal of Medicinal Chemistry, 1988 ,  vol. 31,  # 6  p. 1063 - 1064

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Citation Number: 98

Abstract

Sir: 1-pD-Arabinofuranosylcytosine (ara-C, la) is one of the most potent drugs for the treatment of acute human leukemia.'However, ara-C has several drawbacks; its half-life is very short because of deamination to chemotherapeutically inactive 1-pD- arabinofuranosyluracil by cytidine deaminase, and it is not effective against solid tumors. In order to overcome these problems, efforts have been made to develop prodrugs3 or ...