Journal of Medicinal Chemistry p. 1774 - 1779 (1987)
Update date:2022-08-04
Topics: Total synthesis Structure-Activity Correlations Antileukemic activity Ring a substituted Camptothecin analogues
Wani
Nicholas
Manikumar
Wall
Nineteen racemic ring A substituted analogues of the antitumor agent 20(S)-camptothecin were prepared by total synthesis and evaluated for in vitro cytotoxic activity against KB cell culture and in vivo antileukemic activity against L1210. These compounds bore a wide variety of substitutents at C11 designed to confer upon the ring system a broad range of combinations of electronic, steric, and lipophilic effects. A few C10-substituted derivatives as well as C10,C11-disubstituted analogues prepared as part of a concurrent study have also been included for general comparison. With the notable exception of the cyano derivative, the 11-substituted compounds displayed only modest in vitro and in vivo activities, and there was a remarkable insensitivity toward the nature of the substituent. In contrast, the 9- and 10-substituted compounds exhibited a considerably higher level of dose potency and activity both in vitro and in vitro.
View MoreSEA BRGIHT INDUSTRY CO.,LIMITED
Contact:0086 755 8622 3990
Address:Rm 17B3,GuangCaiXinTianDi Bldg,GuiMiao Rd,NanShan District,Shenzhen,China
Changzhou Anyi Biochem Co., Ltd.
Contact:+86-519-88836158
Address:no,51 caoda
AUSHUN PHARMACEUTICAL TECHNOLOGY CO,.LTD
Contact:+86-25-86883560 15951806178
Address:14 Dayingbi, Zhujiang Rd. East, Nanjing, Jiangsu, China.
Shanghai Yudiao Chemistry Technology Co.,Ltd
Contact:0086-18964703211
Address:Building NO.5, NO.218,Rongtian Road,ganxiang town,Jinshan District,shanghai,201518,china
Changzhou Qidi Chemical Co., Ltd
website:http://www.czqdhg.com/
Contact:86-519-83382137
Address:128-1-16# HuaYuan Street,Hutang Town,Wujin District,Changzhou City,P.R.China.
Doi:10.1007/s11094-018-1729-1
(2018)Doi:10.3987/COM-08-11421
(2008)Doi:10.1007/s10870-011-0243-z
(2012)Doi:10.1248/cpb.34.3635
(1986)Doi:10.1080/10426507.2020.1858081
(2020)Doi:10.1016/S0040-4039(00)95657-0
(1987)