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.
View MoreContact:18710867521(wechat)
Address:Rm10516,Galaxy Tech Building #2,No.25 Tangyan Rd,Hi-Tech Zone,Xi'an, China
TIANJIN DONGRUXIANG MINERALS MARKETING CO.,LTD(expird)
Contact:22-58516360
Address:tianjin
Contact:86-571-61063068
Address:LINAN
Sichuan Sangao Biochemical Co., Ltd
Contact:+86-28-84874233
Address:19F, Bldg.2, Shudu Center, Tianfu 2nd St., Hi-tech zone, Chengdu 610041, Sichuan Province, China.
Xi'an caijing Opto-Electrical Science & Technology Co., LTD
Contact:+86-29-88294447
Address:NO.168 Zhangba Rd. East, Xi'an, P.R.China
Doi:10.1021/ja001656v
(2000)Doi:10.1016/S0020-1693(00)84380-7
(1987)Doi:10.1021/ja01481a052
(1961)Doi:10.1021/jo01052a067
(1962)Doi:10.1246/bcsj.66.251
(1993)Doi:10.1021/ja01221a040
(1945)
