Journal of Medicinal Chemistry p. 862 - 865 (1986)
Update date:2022-08-04
Topics:
Lin, Tai-Shun
Brubaker, William F.
Wang, Zi-Hou
Park, Susanna
Prusoff, William H.
The (chloroethyl)nitrosourea analogues of 2'-deoxyuridine and 2'-deoxy-5-fluorouridine, 3'-<3-(2-chloroethyl)-3-nitrosoureido>-2',3'-dideoxyuridine (3'-CdUNU, 7) and 3'-<3-(2-chloroethyl)-3-nitrosoureido>-2',3'-dideoxy-5-fluorouridine (3'-CFdUNU, 8), have been synthesized by treatment of the corresponding 3'-amino nucleosides with chloroethyl isocyanate, followed by nitrosation of the resulting ureas.Nucleoside nitrosoureas 7 and 8 exhibited marked anticancer activity against L1210 leukemia in tumor-bearing mice.At an optimum dosage level of 40 mg/kg, 7 and 8 produced 90percent and 60percent "cures" (>60-day survivors), respectively.The structure-activity relationships are discussed.
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