Bioorganic and Medicinal Chemistry Letters p. 1887 - 1892 (1996)
Update date:2022-08-03
Topics:
Matsuda, Akira
Hattori, Hideshi
Tanaka, Motohiro
Sasaki, Takuma
1-(3-C-ethynyl-β-D-ribo-pentofuranosyl)uracil (EUrd) has been designed as a potential multifunctional antitumor nucleoside antimetabolite. EUrd was synthesized by condensation of 1-O-acetyl-2,3,5-tri-O-benzoyl-3-C-ethynyl-α,β-D-ribo-pentofuranose (6) and bis(trimethylsilyl)uracil in the presence of trimethylsilyl triflate in CH3CN in good yield, followed by debenzoylation with NH3/MeOH. In vitro tumor cell growth inhibitory activity of EUrd against 14 human solid tumor cell lines was compared with 5-fluorouridine (FUrd), 2'-deoxy-5-fluorouridine (FdUrd), and 5-fluorouracil (5-FU) as positive controls. EUrd was a quite potent tumor cell growth inhibitor against almost all the tumor cell lines examined in this study except for human pancreas PANC-1 cells, and the potency of EUrd is about 6 to 650 times stronger than that of 5-FU and comparable to that of FUrd and FdUrd. EUrd showed also potent antitumor activity against human tumors as xenografts in nude mice when given in a daily intravenous dose of 2 mg/kg on consecutive days.
View MoreContact:
Address:No.89,Xinhua Road, Langfang City,Hebei China
Xian Changyue Biological Technology Co., Ltd.
website:https://www.xachangyue.com/
Contact:+86-029-62886900
Address:Keji Road NO.70
Suzhou Sinosun Imp.&Exp. Corporation
website:http://www.szsinosun.com
Contact:+86-512-63488895,63488616
Address:No.758 East Jiangling Road Wujiang Economic & Technological Developmenty Zone Jiangsu China
Mollt Biochem Co., Ltd(expird)
Contact:+86-21-38682181
Address:shanghai ,china
Nanjing Spring & Autumn Biological Engineering Co., Ltd.
Contact:86-180510-83338
Address:Suite# 210, No. 1 BuildingNanjing Agricultural Biotechnology High-tech Entrepreneurship Center, No. 4 Tongwei Road, Xuanwu District, Nanjing,China
Doi:10.1021/ja01311a021
(1935)Doi:10.1039/b507752d
(2005)Doi:10.1021/jo00870a010
(1976)Doi:10.1515/chempap-2015-0027
(2015)Doi:10.1016/S0960-894X(03)00381-0
(2003)Doi:10.1021/jo00874a007
(1976)